标签归档：cid

CID44216842(Synonyms: Cdc42-IN-1)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID44216842 (Synonyms: Cdc42-IN-1) 纯度: 99.84%

CID44216842 (Cdc42-IN-1) 是一种有效的选择性 Cdc42 抑制剂。在 GTP 结合测定中，CID44216842 对 Cdc42 野生型和 Cdc42Q61L 突变型的 EC50 分别为 1.0 和 1.2 μM。在 GDP 结合测定中，CID44216842 对 Cdc42 野生型和 Cdc42Q61L 突变型的 EC50 分别为 0.3 和 0.5 μM。可用作分子探针。

CID44216842(Synonyms: Cdc42-IN-1)

CID44216842 Chemical Structure

CAS No. : 1222513-26-9

规格 价格 是否有货 数量
5 mg ￥1000 In-stock
10 mg ￥1700 In-stock
25 mg ￥3500 In-stock
50 mg ￥5500 In-stock
100 mg ￥9500 In-stock
200 mg   询价  
500 mg   询价  

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CID44216842 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Ferroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe[1].

IC50 & Target

EC50: 1.0 μM (Cdc42 WT, in GTP binding assay) and 1.2 μM (Cdc42Q61L mutant, in GTP binding assay)[1]
EC50: 0.3 μM (Cdc42 WT, in GDP binding assay) and 0.5 μM (Cdc42Q61L mutant, in GDP binding assay)[1]
体外研究
(In Vitro)

CID44216842 inhibits GTP binding to both Cdc42 and its mutant in a dose-dependent manner. The inhibition is specific toward Cdc42 with no effects on other GTPases including Rac and Rho in the same family[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

486.38

Formula

C22H20BrN3O3S
CAS 号

1222513-26-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (514.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0560 mL 10.2800 mL 20.5601 mL
5 mM 0.4112 mL 2.0560 mL 4.1120 mL
10 mM 0.2056 mL 1.0280 mL 2.0560 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.28 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Lin Hong, et al. Characterization of a Cdc42 Protein Inhibitor and Its Use as a Molecular Probe. J Biol Chem. 2013 Mar 22;288(12):8531-43.

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CID-2858522

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID-2858522  纯度: 95.52%

CID-2858522 是一种高效的选择性抗原受体介导的 NF-κB 抑制剂，IC50 为 70 nM。

CID-2858522

CID-2858522 Chemical Structure

CAS No. : 758679-97-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥616 In-stock
5 mg ￥560 In-stock
10 mg ￥1000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

CID-2858522 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Obesity Compound Library
  • Transcription Factor Targeted Library
  • Anti-Liver Cancer Compound Library

生物活性

CID-2858522 is a highly potent and selective antigen receptor-mediated NF-κB activation inhibitor with an IC50 of 70 nM.

IC50 & Target[1]

NF-κB

70 nM (IC50)

体外研究
(In Vitro)

CID-2858522 (Compound 1) inhibits antigen receptor-mediated NF-κB with an IC50 of 70 nM. CID-2858522 also inhibits testosterone hydroxylase in the presence of human liver microsomes (HLM) and an NADPH generating system with an IC50 of 85 μM[1]. In the HEK293 cell line used for primary screening, CID-2858522 suppresses NF-κB reporter gene activity in a concentration-dependent manner, with IC50 ~70 nM and with maximum inhibition achieved at 0.25-0.5 μM. In contrast, CID-2858522 does not inhibit TNF-induced NF-κB-reporter gene activity at concentrations as high as 4 μM, thus demonstrating selectivity for the NF-κB pathway activated by PMA/Ionomycin. Cell viability assays indicate that CID-2858522 is not toxic to HEK293 cells at concentrations ≤8 μM. CID-2858522 also potently inhibits PMA/Ionomycin-induced NF-κB reporter gene activity in transient transfection assays[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In vivo dose-exposure profiling of CID-2858522 (Compound 1a) is conducted using a small cohort of three male mice. CID-2858522 exhibits nonlinear pharmacokinetics, showing higher serum levels at the 0.5 h measurement time for the 30 mg/kg dose compared to 50 mg/kg but displaying typical dose-dependent behavior when measured at t=3 h. The increasing accumulation seen at a dose of 50 mg/kg may be due to a depot effect created by CYP3A4 inhibition. The cohort exhibits clear signs of morbidity at t=3 h at the 50 mg/kg dose[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

465.63

Formula

C28H39N3O3
CAS 号

758679-97-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (53.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1476 mL 10.7381 mL 21.4763 mL
5 mM 0.4295 mL 2.1476 mL 4.2953 mL
10 mM 0.2148 mL 1.0738 mL 2.1476 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.37 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.37 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.37 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Okolotowicz KJ, et al. Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activationpathway. Bioorg Med Chem. 2010 Mar 1;18(5):1918-24.

    [2]. Peddibhotla S, et al. Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules. J Med Chem. 2010 Jun 24;53(12):4793-7.

    [3]. Shi R, et al. Chemical biology strategy reveals pathway-selective inhibitor of NF-kappaB activation induced by protein kinase C. ACS Chem Biol. 2010 Mar 19;5(3):287-99.
Cell Assay
[2]

Cell viability is estimated based on cellular ATP levels, measured using ATPlite kit. HEK293 cells at a density of 105/mL are seeded at 90 μL per well in 96-well white plates and cultured overnight. Compounds (e.g., CID-2858522; 1 μM, 2 μM, 3 μM, and 4 μM) are added (5 μL in medium) to wells and cells are cultured for 16 h, Finally, 50 μL ATPlite solution is added to each well and luminescence activity is read using a luminometer[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
Three male mice are subjected to CID-2858522 (single ip doses at 10, 30, and 50 mg/kg). Blood is drawn at 0.5 and 3 h, and subsequent LC/MS analysis of pooled samples is performed to determine the overall blood levels of CID-2858522.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Okolotowicz KJ, et al. Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activationpathway. Bioorg Med Chem. 2010 Mar 1;18(5):1918-24.

    [2]. Peddibhotla S, et al. Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules. J Med Chem. 2010 Jun 24;53(12):4793-7.

    [3]. Shi R, et al. Chemical biology strategy reveals pathway-selective inhibitor of NF-kappaB activation induced by protein kinase C. ACS Chem Biol. 2010 Mar 19;5(3):287-99.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CID5721353

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID5721353  纯度: ≥98.0%

CID5721353 是一种 BCL6 抑制剂，IC50 为 212 μM，Ki 值为 147 μM。

CID5721353

CID5721353 Chemical Structure

CAS No. : 301356-95-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥905 In-stock
2 mg ￥500 In-stock
5 mg ￥900 In-stock
10 mg ￥1500 In-stock
25 mg ￥2900 In-stock
50 mg ￥4900 In-stock
100 mg ￥8400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CID5721353 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

CID5721353 is an inhibitor of BCL6 with an IC50 value of 212 μM, which corresponds to a Ki of 147 μM.

IC50 & Target

IC50: 212 μM (BCL6)[1]
Ki: 147 μM(BCL6)[1]
体外研究
(In Vitro)

BCL6 is a member of the BTB/POZ family of transcription factors. CID5721353 (Compound 79-6) specifically inhibits BCL6 repressor activity. CID5721353 disrupts BCL6 transcriptional complexes and reactivates BCL6 target genes. CID5721353 can specifically kill primary human DLBCL cells. Fifteen of 19 BCL6-positive cases (79%) display greater than 25% loss of viability in response to CID5721353 at 125 or 250 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In order to test whether CID5721353 (Compound 79-6) can perform as an anti-lymphoma therapeutic agent in vivo, whether it can penetrate tumors after parenteral administration through a distal site is determined. For this purpose 107OCI-Ly7 cells are injected into the right flank of 10 SCID mice and allowed to form tumors. Once tumors reach ~1.5 grams, animals are injected IP with a single dose of 50 mg/kg of CID5721353 in 10% DMSO or vehicle (10% DMSO) and sacrificed at 0.5, 1, 1.5, 3, 6, 12 and 24 hours after CID5721353 administration. Blood and tumors are harvested. Quantitative HPLC/MS analysis of the serum shows that CID5721353 levels peak (to 55 μg/mL, which is equivalent to a 122 μM concentration) one hour after the IP injection. CID5721353 also reaches its highest peak (24.5 ng/mg) at the 1-hour time point in the tumors, and after a sharp decline in levels, decreases gradually over 24 hours[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

457.28

Formula

C15H9BrN2O6S2
CAS 号

301356-95-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (109.34 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1868 mL 10.9342 mL 21.8684 mL
5 mM 0.4374 mL 2.1868 mL 4.3737 mL
10 mM 0.2187 mL 1.0934 mL 2.1868 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.47 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.47 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cerchietti LC, et al. A small-molecule inhibitor of BCL6 kills DLBCL cells in vitro and in vivo. Cancer Cell. 2010 Apr 13;17(4):400-11.
Cell Assay
[1]

Cell number and viability are determined by an EB/AO-based method and cells are cultivated in medium containing 80% RPMI and 20% human serum supplemented with antibiotics, L-glutamine and HEPES for 48 h. Pimary human diffuse large B cell lymphoma (DLBCL) cells are exposed to 125 and 250 μM of CID5721353 or control (DMSO) in triplicates. After 48 h of exposure viability is determined by using an ATP-based luminescent method and EB/AO. Specimens with 20% or higher loss of viability in the controls are discarded[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Six to eight-week old male SCID mice are subcutaneously injected in the left flank with low-passage 107 human OCI-Ly7 cells. When tumors reach 1500 mm3 the mice are IP injected with 50 mg/kg of CID5721353 in DMSO (n=8) or DMSO (control, n=2). Blood and tumors are harvested at different time points after injection (30 min, 1 h, 1.5 h, 3 h, 6 h, 12 h and 24 h)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Cerchietti LC, et al. A small-molecule inhibitor of BCL6 kills DLBCL cells in vitro and in vivo. Cancer Cell. 2010 Apr 13;17(4):400-11.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

ML230(Synonyms: CID44640177; SID 88095709)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ML230 (Synonyms: CID44640177; SID 88095709) 纯度: 99.12%

ML230 (CID44640177; SID 88095709) 是一种 ATP 结合转运因亚型 ABCG2 的选择性抑制剂， 对 ABCG2 的抑制作用是 ABCB1 的 36 倍，EC50 值分别为 0.13 μM 和 4.65 μM。

ML230(Synonyms: CID44640177; SID 88095709)

ML230 Chemical Structure

CAS No. : 1776055-05-0

规格 价格 是否有货 数量
5 mg ￥2800 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

ML230 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Membrane Transporter/Ion Channel Compound Library
  • Anti-Cancer Compound Library
  • Lipid Metabolism Compound Library

生物活性

ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively[1].

IC50 & Target

EC50: ABCG2 (0.13 μM)[1]
分子量

439.47

Formula

C25H21N5O3
CAS 号

1776055-05-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (75.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2755 mL 11.3773 mL 22.7547 mL
5 mM 0.4551 mL 2.2755 mL 4.5509 mL
10 mM 0.2275 mL 1.1377 mL 2.2755 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.69 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Strouse JJ, et al. Selective Efflux Inhibition of ATP-binding Cassette Sub-family G Member 2. Probe Reports from the NIH Molecular Libraries Program. November 30, 2010.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CID 2011756

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID 2011756  纯度: 96.04%

CID 2011756 是一种广谱的，ATP 竞争性的 PKD 抑制剂，对 PKD1 的 IC50 值为 3.2 µM，在细胞中对 PKD2 和 PKD3 的 IC50 值分别为 0.6 和 0.7 µM；CID 2011756 同时具有抗肿瘤活性。

CID 2011756

CID 2011756 Chemical Structure

CAS No. : 638156-11-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥900 In-stock
50 mg ￥3000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CID 2011756 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library

生物活性

CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.

IC50 & Target[1]

Cellular PKD2

0.6 μM (IC50)

Cellular PKD3

0.7 μM (IC50)

PKD1

3.2 μM (IC50)

体外研究
(In Vitro)

CID 2011756 is an ATP-competitive PKD1 inhibitor, with an IC50 of 3.2 µM. CID 2011756 decreases the phosphorylation of endogenous PKD1 Ser916 in LNCaP cancer cells with an EC50 of 10±0.7 µM. CID 2011756 also has cellular pan-PKD inhibitory effects, with IC50s of 0.6±0.1 µM and 0.7±0.2 µM for PKD2 and PKD3, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

396.87

Formula

C22H21ClN2O3
CAS 号

638156-11-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 20 mg/mL (50.39 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5197 mL 12.5986 mL 25.1972 mL
5 mM 0.5039 mL 2.5197 mL 5.0394 mL
10 mM 0.2520 mL 1.2599 mL 2.5197 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2 mg/mL (5.04 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (5.04 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (5.04 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (5.04 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Sharlow ER, et al. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CID 5951923

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID 5951923 

CID 5951923是一种有效的 Krüppel-like factor 5 (KLF5) 抑制剂，IC50 值为 603 nM，CID 5951923 可在体外抑制癌细胞的增殖。

CID 5951923

CID 5951923 Chemical Structure

CAS No. : 749872-43-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro[1].

IC50 & Target

IC50: 603 nM (KLF5)[1]
体外研究
(In Vitro)

CID 5951923 (1 nM-100 μM; 48 h) inhibits proliferation of DLD-1 cells in a dose-dependent manner[1].
CID 5951923 (10 μM; 24 h) significantly decreases endogenous KLF5 levels in the DLD-1 cells, increases phosphorylation levels of pEGFFpY1068, and downregulated EGR1[1].
CID 5951923 (10 μM) inhibits proliferation of cancer cell lines mainly in highly express KLF5 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: DLD-1 and IEC-6 cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 48 h
Result: Inhibited proliferation of DLD-1 cells with an IC50 of 1.6 μM.

分子量

382.39

Formula

C16H18N2O7S
CAS 号

749872-43-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Bialkowska AB, et, al. Identification of small-molecule inhibitors of the colorectal cancer oncogene Krüppel-like factor 5 expression by ultrahigh-throughput screening. Mol Cancer Ther. 2011 Nov; 10(11): 2043-51.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CID 5951923

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID 5951923 

CID 5951923是一种有效的 Krüppel-like factor 5 (KLF5) 抑制剂，IC50 值为 603 nM，CID 5951923 可在体外抑制癌细胞的增殖。

CID 5951923

CID 5951923 Chemical Structure

CAS No. : 749872-43-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro[1].

IC50 & Target

IC50: 603 nM (KLF5)[1]
体外研究
(In Vitro)

CID 5951923 (1 nM-100 μM; 48 h) inhibits proliferation of DLD-1 cells in a dose-dependent manner[1].
CID 5951923 (10 μM; 24 h) significantly decreases endogenous KLF5 levels in the DLD-1 cells, increases phosphorylation levels of pEGFFpY1068, and downregulated EGR1[1].
CID 5951923 (10 μM) inhibits proliferation of cancer cell lines mainly in highly express KLF5 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: DLD-1 and IEC-6 cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 48 h
Result: Inhibited proliferation of DLD-1 cells with an IC50 of 1.6 μM.

分子量

382.39

Formula

C16H18N2O7S
CAS 号

749872-43-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Bialkowska AB, et, al. Identification of small-molecule inhibitors of the colorectal cancer oncogene Krüppel-like factor 5 expression by ultrahigh-throughput screening. Mol Cancer Ther. 2011 Nov; 10(11): 2043-51.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CID 5951923

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID 5951923 

CID 5951923是一种有效的 Krüppel-like factor 5 (KLF5) 抑制剂，IC50 值为 603 nM，CID 5951923 可在体外抑制癌细胞的增殖。

CID 5951923

CID 5951923 Chemical Structure

CAS No. : 749872-43-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro[1].

IC50 & Target

IC50: 603 nM (KLF5)[1]
体外研究
(In Vitro)

CID 5951923 (1 nM-100 μM; 48 h) inhibits proliferation of DLD-1 cells in a dose-dependent manner[1].
CID 5951923 (10 μM; 24 h) significantly decreases endogenous KLF5 levels in the DLD-1 cells, increases phosphorylation levels of pEGFFpY1068, and downregulated EGR1[1].
CID 5951923 (10 μM) inhibits proliferation of cancer cell lines mainly in highly express KLF5 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: DLD-1 and IEC-6 cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 48 h
Result: Inhibited proliferation of DLD-1 cells with an IC50 of 1.6 μM.

分子量

382.39

Formula

C16H18N2O7S
CAS 号

749872-43-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Bialkowska AB, et, al. Identification of small-molecule inhibitors of the colorectal cancer oncogene Krüppel-like factor 5 expression by ultrahigh-throughput screening. Mol Cancer Ther. 2011 Nov; 10(11): 2043-51.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

VU0359595(Synonyms: CID-53361951; ML-270)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

VU0359595 (Synonyms: CID-53361951; ML-270)

VU0359595 (CID-53361951; ML-270) 是一种选择性磷脂酶 D1 (PLD1) 抑制剂，IC50 值为 3.7 nM。VU0359595 对 PLD1 的选择性比 PLD2 (IC50=6.4 μM) 高 1700 倍以上。VU0359595 可用于癌症、糖尿病、神经退行性疾病和炎性疾病等疾病研究。

VU0359595(Synonyms: CID-53361951; ML-270)

VU0359595 Chemical Structure

CAS No. : 1246303-14-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases[1][2][3][4].

IC50 & Target[1]

PLD1

3.7 nM (IC50)

PLD2

6.4 μM (IC50)

体外研究
(In Vitro)

VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells[2].
VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2].
VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [3H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells[3].
VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4].
VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

497.43

Formula

C25H29BrN4O2
CAS 号

1246303-14-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009;19(7):1916-1920.

    [2]. Burkhardt U, et al. Phospholipase D is a target for inhibition of astroglial proliferation by ethanol. Neuropharmacology. 2014;79:1-9.

    [3]. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019;184:243-257.

    [4]. Bermúdez V, et al. Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. Front Cell Neurosci. 2019;13:154. Published 2019 Apr 24.

    [5]. Jia X, et al. Gliotoxin promotes Aspergillus fumigatus internalization into type II human pneumocyte A549 cells by inducing host phospholipase D activation. Microbes Infect. 2014 Jun;16(6):491-501.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

VU0359595(Synonyms: CID-53361951; ML-270)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

VU0359595 (Synonyms: CID-53361951; ML-270)

VU0359595 (CID-53361951; ML-270) 是一种选择性磷脂酶 D1 (PLD1) 抑制剂，IC50 值为 3.7 nM。VU0359595 对 PLD1 的选择性比 PLD2 (IC50=6.4 μM) 高 1700 倍以上。VU0359595 可用于癌症、糖尿病、神经退行性疾病和炎性疾病等疾病研究。

VU0359595(Synonyms: CID-53361951; ML-270)

VU0359595 Chemical Structure

CAS No. : 1246303-14-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases[1][2][3][4].

IC50 & Target[1]

PLD1

3.7 nM (IC50)

PLD2

6.4 μM (IC50)

体外研究
(In Vitro)

VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells[2].
VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2].
VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [3H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells[3].
VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4].
VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

497.43

Formula

C25H29BrN4O2
CAS 号

1246303-14-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009;19(7):1916-1920.

    [2]. Burkhardt U, et al. Phospholipase D is a target for inhibition of astroglial proliferation by ethanol. Neuropharmacology. 2014;79:1-9.

    [3]. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019;184:243-257.

    [4]. Bermúdez V, et al. Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. Front Cell Neurosci. 2019;13:154. Published 2019 Apr 24.

    [5]. Jia X, et al. Gliotoxin promotes Aspergillus fumigatus internalization into type II human pneumocyte A549 cells by inducing host phospholipase D activation. Microbes Infect. 2014 Jun;16(6):491-501.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

VU0359595(Synonyms: CID-53361951; ML-270)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

VU0359595 (Synonyms: CID-53361951; ML-270)

VU0359595 (CID-53361951; ML-270) 是一种选择性磷脂酶 D1 (PLD1) 抑制剂，IC50 值为 3.7 nM。VU0359595 对 PLD1 的选择性比 PLD2 (IC50=6.4 μM) 高 1700 倍以上。VU0359595 可用于癌症、糖尿病、神经退行性疾病和炎性疾病等疾病研究。

VU0359595(Synonyms: CID-53361951; ML-270)

VU0359595 Chemical Structure

CAS No. : 1246303-14-9

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生物活性

VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases[1][2][3][4].

IC50 & Target[1]

PLD1

3.7 nM (IC50)

PLD2

6.4 μM (IC50)

体外研究
(In Vitro)

VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells[2].
VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2].
VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [3H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells[3].
VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4].
VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

497.43

Formula

C25H29BrN4O2
CAS 号

1246303-14-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009;19(7):1916-1920.

    [2]. Burkhardt U, et al. Phospholipase D is a target for inhibition of astroglial proliferation by ethanol. Neuropharmacology. 2014;79:1-9.

    [3]. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019;184:243-257.

    [4]. Bermúdez V, et al. Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. Front Cell Neurosci. 2019;13:154. Published 2019 Apr 24.

    [5]. Jia X, et al. Gliotoxin promotes Aspergillus fumigatus internalization into type II human pneumocyte A549 cells by inducing host phospholipase D activation. Microbes Infect. 2014 Jun;16(6):491-501.

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ML-098(Synonyms: CID-7345532)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ML-098 (Synonyms: CID-7345532) 纯度: 99.98%

ML-098（CID-7345532）是GTP结合蛋白Rab7的激活剂，EC50值为77.6nM。

ML-098(Synonyms: CID-7345532)

ML-098 Chemical Structure

CAS No. : 878978-76-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥770 In-stock
5 mg ￥700 In-stock
10 mg ￥1200 In-stock
25 mg ￥2550 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

ML-098 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Ferroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library

生物活性

ML-098 (CID-7345532) is an activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM.

IC50 & Target

EC50: 77.6 nM (Rab7)[1]
体外研究
(In Vitro)

Probe compound mL098 (CID-7345532) functions by increasing the affinity of the GTPases for guanine nucleotides, leading to the hypothesis that these activators interact with GTPases bind to an allosteric binding site localized between switch regions I and II. ML-098 is an activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM which shows selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC50s = 588.8, 346.7, 158.5, and 794.3 nM, respectively)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

309.36

Formula

C19H19NO3
CAS 号

878978-76-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (323.25 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2325 mL 16.1624 mL 32.3248 mL
5 mM 0.6465 mL 3.2325 mL 6.4650 mL
10 mM 0.3232 mL 1.6162 mL 3.2325 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

ML216(Synonyms: CID-49852229)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ML216 (Synonyms: CID-49852229) 纯度: 99.89%

ML216 (CID-49852229) 是一种有效，选择性，细胞渗透性的 BLM 解旋酶抑制剂，对 BLMfull-length 和 BLM636-1298 的 IC50 分别为 2.98 μM 和 0.97 μM。ML216 以 Ki 为 1.76 µM 来抑制 BLM 的 ssDNA 依赖性 ATPase 的活性。ML216 具有抗肿瘤活性。

ML216(Synonyms: CID-49852229)

ML216 Chemical Structure

CAS No. : 1430213-30-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605 In-stock
5 mg ￥550 In-stock
10 mg ￥980 In-stock
25 mg ￥1980 In-stock
50 mg ￥3000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

ML216 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library

生物活性

ML216 (CID-49852229) is a potent, selective and cell permeable inhibitor of the DNA unwinding activity of BLM helicase with IC50s of 2.98 μM and 0.97 μM for BLMfull-length and BLM636-1298, respectively. ML216 inhibits ssDNA-dependent ATPase activity of BLM with a Ki of 1.76 µM. Antitumor avtivity[1][2].

IC50 & Target

IC50: 2.98 μM (BLMfull-length) and 0.97 μM (BLM636-1298)[1]
体外研究
(In Vitro)

ML216 (12.5-50 µM; 24-72 hours; PSNG5 and PSNG13cells) treatment inhibits the proliferation of PSNF5 cells in a concentration-dependent manner, but not of PSNG13 cells[1].
ML216 treatment leads to a statistically significant increase in the frequency of sister chromatid exchanges (SCEs) in PSNF5 cells, but not in PSNG13 cells[1].
ML216 increases the sensitivity of PSNF5 cells to aphidicolin but has no sensitizing effect on isogenic PSNG13 cells devoid of BLM[1].
ML216 inhibits both the full length WRN (IC50 of 5 μM) and a truncated WRN500-946 (IC50 of 12.6 μM), with the former being 2.5-fold more sensitive to inhibition. BLM is a little more sensitive than WRN to inhibition by ML216 (1.7-fold based on IC50 values). Despite the detectable inhibition of WRN by ML216, this compound appears selective for BLM in human cells. ML216 inhibits proliferation of WRN+ and WRN− cells equally well, and similarly sensitized both cell types to aphidicolin[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: PSNG5 and PSNG13cells
Concentration: 12.5 μM or 50 µM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Inhibited the proliferation of PSNF5 cells, but not of PSNG13 cells, and did so in a concentration-dependent manner.

体内研究
(In Vivo)

Although ML216 inhibits unwinding by the sequence-related BLM and WRN helicases similarly in vitro, the apparent dependence on BLM for ML216 to exert its biological effects in human cells suggests BLM specificity for the drug’s mechanism of action in vivo. A co-crystal structure of BLM in complex with inhibitor would be informative. Cellular cues in vivo may induce a specific conformation of WRN that makes it resistant to ML216[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

383.32

Formula

C15H9F4N5OS
CAS 号

1430213-30-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 20 mg/mL (52.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6088 mL 13.0439 mL 26.0879 mL
5 mM 0.5218 mL 2.6088 mL 5.2176 mL
10 mM 0.2609 mL 1.3044 mL 2.6088 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (5.22 mM); Suspended solution; Need ultrasonic

    此方案可获得 2 mg/mL (5.22 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Nguyen GH, et al. A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells. Chem Biol. 2013 Jan 24;20(1):55-62.

    [2]. Banerjee T, et al. A new development in DNA repair modulation: discovery of a BLM helicase inhibitor. Cell Cycle. 2013 Mar 1;12(5):713-4.

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ML141(Synonyms: CID-2950007)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ML141 (Synonyms: CID-2950007) 纯度: 99.71%

ML141 (CID-2950007) 是一种高效、变构、选择性、可逆的 Cdc42 GTPase 非竞争性抑制剂。ML141 抑制 Cdc42 野生型和 Cdc42 Q61L 突变体的 EC50 值分别为 2.1 和 2.6 μM。ML141 对 GTPases Rho 家族的其他成员 (Rac1, Rab2, Rab7) 表现出低的微极性和选择性。ML141 在多个细胞系中没有显示细胞毒性。

ML141(Synonyms: CID-2950007)

ML141 Chemical Structure

CAS No. : 71203-35-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥770 In-stock
5 mg ￥700 In-stock
10 mg ￥1200 In-stock
50 mg ￥4500 In-stock
100 mg ￥7200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

ML141 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • GPCR/G Protein Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Peptidomimetic Library
  • Ferroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines[1][2].

体外研究
(In Vitro)

ML141 (CID-2950007) is not cytotoxic in either cell line at doses of 0.1-3 μM after treatment for 4 days. OVCA429 cells were insensitive to 10 μM compound, whereas some cytotoxicity was observed in SKOV3ip cells at this concentration after a 4-day treatment, although it did not reach statistical significance. ML141 is not cytotoxic toward Swiss 3T3 or Vero E6 cells up to 10 μM for 24 and 48 h, respectively[1].
ML141 inhibits 3T3 fibroblast filopodia formation, and inhibits ovarian cancer cell migration[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

ML141 (CID-2950007) (10 µM; intracerebroventricular injection) causes acute anxiety in mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl/6J mice[3]
Dosage: 10 µM
Administration: Intracerebroventricular injection
Result: Increased anxiety in mice.

分子量

407.49

Formula

C22H21N3O3S
CAS 号

71203-35-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 55 mg/mL (134.97 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4540 mL 12.2702 mL 24.5405 mL
5 mM 0.4908 mL 2.4540 mL 4.9081 mL
10 mM 0.2454 mL 1.2270 mL 2.4540 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (5.10 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.10 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.10 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.10 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Hong L, et al. Characterization of a Cdc42 protein inhibitor and its use as a molecular probe. J Biol Chem. 2013 Mar 22;288(12):8531-43.

    [2]. Surviladze Z, et al. A Potent and Selective Inhibitor of Cdc42 GTPase. Probe Reports from the NIH Molecular Libraries Program

    [3]. Hanin G, et al. Competing targets of microRNA-608 affect anxiety and hypertension. Hum Mol Genet. 2014 Sep 1;23(17):4569-80.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CID755673

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID755673  纯度: 99.12%

CID755673是高效选择性的PKD1抑制剂，IC50 of 值为182 nM。

CID755673

CID755673 Chemical Structure

CAS No. : 521937-07-5

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥660 In-stock
5 mg ￥600 In-stock
10 mg ￥900 In-stock
50 mg ￥2500 In-stock
100 mg ￥4500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CID755673 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Targeted Diversity Library

生物活性

CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.

IC50 & Target[1]

PKD1

182 nM (IC50)

PKD3

227 nM (IC50)

PKD2

280 nM (IC50)

体外研究
(In Vitro)

CID755673 blocks phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. CID755673 inhibits the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. CID755673 inhibits prostate cancer cell proliferation, cell migration, and invasion[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Acute administration of the PKD inhibitor CID755673 to normal mice reduces both PKD1 and 2 phosphorylation in a time and dose-dependent manner. Chronic CID755673 administration to T2D db/db mice for two weeks reduces expression of the gene expression signature of PKD activation, enhances indices of both diastolic and systolic left ventricular function and is associated with reduced heart weight[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

217.22

Formula

C12H11NO3
CAS 号

521937-07-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (460.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.6036 mL 23.0181 mL 46.0363 mL
5 mM 0.9207 mL 4.6036 mL 9.2073 mL
10 mM 0.4604 mL 2.3018 mL 4.6036 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.51 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.51 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.51 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Sharlow ER, et al. Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone. J Biol Chem. 2008 Nov 28;283(48):33516-26.

    [2]. Venardos K, et al. The PKD inhibitor CID755673 enhances cardiac function in diabetic db/db mice. PLoS One. 2015 Mar 23;10(3):e0120934.
Kinase Assay
[1]

The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μL of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

The wound-induced migration is triggered by scraping the cells with a plastic pipette tip, and the wound is imaged immediately. The DU145 cells are then are treated with or without CID755673 at different concentrations. The wound is imaged immediately (0 h) and at different intervals with an inverted phase-contrast microscope with a ×10 objective. At the end of the assay, cells are fixed with methanol and stained with crystal violet for a final image[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: For acute inhibitor studies, C57BL6 mice are administered a single dose of vehicle (5% DMSO in PBS, pH 7.4), or the selective PKD inhibitor CID755673 at 1 or 10mg/kg body weight. Mice are killed one or four hr later and heart collected for later analysis. For chronic inhibitor experiments, 8-week old db/db mice receives vehicle or CID755673 at 1 or 10mg/kg bodyweight for 16 days, by daily intraperitoneal (i.p.) injection[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Sharlow ER, et al. Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone. J Biol Chem. 2008 Nov 28;283(48):33516-26.

    [2]. Venardos K, et al. The PKD inhibitor CID755673 enhances cardiac function in diabetic db/db mice. PLoS One. 2015 Mar 23;10(3):e0120934.

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ML228(Synonyms: CID-46742353)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ML228 (Synonyms: CID-46742353) 纯度: ≥98.0%

ML228 (CID-46742353) 是一种有效的 HIF 信号通路激活剂，EC50 为 1 μM。ML228 可激活 HIF 以及下游 EGFR。

ML228(Synonyms: CID-46742353)

ML228 Chemical Structure

CAS No. : 1357171-62-0

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1089 In-stock
5 mg ￥990 In-stock
10 mg ￥1750 In-stock
50 mg ￥7200 In-stock
100 mg ￥11200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

ML228 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library

生物活性

ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF[1][2].

IC50 & Target

EC50: 1 μM (HIF)[1]
体外研究
(In Vitro)

ML228 (CID-46742353) represents a novel chemotype available to the research community for the study of HIF activation and its therapeutic potential. Not only is the compound substantially different in structure from known HIF activators, ML228 lacks the acidic functional group almost universally present in PHD inhibitors, which may be important for certain disease applications[1][2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

ML228 (injection; 1 µg/kg; 7 days) treatments following spinal cord injury (SCI) improves the local hypoxic ischemia environment, reduce SCI secondary injury and promote the recovery of neurological function[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD rat[3]
Dosage: 1 µg/kg
Administration: injection; 7 days
Result: Alleviated SCI of the central nervous system and relieve associated symptoms.

分子量

415.49

Formula

C27H21N5
CAS 号

1357171-62-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 35 mg/mL (84.24 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4068 mL 12.0340 mL 24.0680 mL
5 mM 0.4814 mL 2.4068 mL 4.8136 mL
10 mM 0.2407 mL 1.2034 mL 2.4068 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.02 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.02 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.02 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Theriault JR, et al. Discovery of a Small Molecule Activator of the Hypoxia Inducible Factor Pathway. Probe Reports from the NIH Molecular Libraries Program.

    [2]. Theriault JR, et al. Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway. Bioorg Med Chem Lett. 2012 Jan 1;22(1):76-81.

    [3]. Chen H, et al. Effect of hypoxia-inducible factor-1/vascular endothelial growth factor signaling pathway on spinal cord injury in rats.Exp Ther Med. 2017 Mar;13(3):861-866.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CID 16020046

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CID 16020046  纯度: 99.92%

CID 16020046 是一种有效的，选择性 GPR55 拮抗剂，抑制 GPR55 的组成型活性，IC50 为 0.15 μM。CID 16020046 抑制 GPR55 介导的 Ca2+ 信号传导和 GPR55 介导的 ERK1/2 磷酸化。CID 16020046 降低了内皮细胞的伤口愈合，并参与了血小板功能的调节。

CID 16020046

CID 16020046 Chemical Structure

CAS No. : 834903-43-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1628 In-stock
10 mg ￥1480 In-stock
50 mg ￥6230 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CID 16020046 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Targeted Diversity Library

生物活性

CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function[1].

体外研究
(In Vitro)

CID 16020046 has weak activities close for inhibition of the acetylcholinesterase (pIC50=4.4), antagonism of the m-opioid receptor (pIC50=4.6), and blockade of KCNH2, the hERG channel (pIC50=4.6) 6 in human embryonic kidney (HEK)-G protein–coupled receptor 55 (GPR55) cells[1].
CID 16020046 (2.5 μM; for ≥25 minutes) significantly inhibits the lysophosphatidylinositol (LPI; 2.5 μM) induced ERK1/2 phosphorylation. CID 16020046 alone fails to induce intracellular Ca2+ release in HEK-GPR55, HEKCB1 cells and shows no ERK1/2 phosphorylation[1].
Pretreatment with CID16020046 (0.01, 0.1, 1, 10 μM) leads to a concentration-dependent decrease in GPR55-mediated NFAT activation, NF-kB activation, and SRE induction in response to 1 μM LPI or GSK319197A in HEKGPR55 and HEK-CB1 cells[1].
CID16020046 (2.5 μM) antagonizes GPR55-mediated activation and nuclear translocation of transcription factors but has no effect on CB1-mediated CREB activation[1].
Pretreatment CID16020046 (1 μM) abolished the LPI-induced stimulation of wound healing in HMVEC-Ls[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line: HEK-CB1 and HEK-CB2 cells[1]
Concentration: 2.5 μM
Incubation Time: For ≥25 minutes
Result: Significantly inhibited the LPI (2.5 μM) induced ERK1/2 phosphorylation.
Treatment alone showed no ERK1/2 phosphorylation and did not alter WIN55,212-2 (2.5 μM) induced ERK1/2 phosphorylation in HEK-CB1 and HEK-CB2 cells.

分子量

425.44

Formula

C25H19N3O4
CAS 号

834903-43-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (235.05 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3505 mL 11.7525 mL 23.5051 mL
5 mM 0.4701 mL 2.3505 mL 4.7010 mL
10 mM 0.2351 mL 1.1753 mL 2.3505 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.88 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kargl J, et al. A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J Pharmacol Exp Ther. 2013 Jul;346(1):54-66.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务