标签归档：cay

CAY10471 Racemate(Synonyms: TM30089 Racemate)

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CAY10471 Racemate (Synonyms: TM30089 Racemate) 纯度: 99.35%

CAY10471 Racemate (TM30089 Racemate) 是一种有效、高度选择性的前列腺素 D2 受体 (CRTH2) 拮抗剂，对 hCRTH2 的 Ki 值为 0.6 nM，对其选择性远高于人血栓素 A2 受体 TP (Ki，>10000 nM) 或 PGD2 受体 DP (Ki，1200 nM)。CAY10471 Racemate 对小鼠和大鼠的同源 CRTH2 也具有拮抗作用。

CAY10471 Racemate(Synonyms: TM30089 Racemate)

CAY10471 Racemate Chemical Structure

CAS No. : 844639-57-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1210 In-stock
5 mg ￥1100 In-stock
10 mg ￥1800 In-stock
25 mg ￥3900 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

CAY10471 Racemate 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Endocrinology Compound Library
  • Angiogenesis Related Compound Library

生物活性

CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2[1].

IC50 & Target[1]

hCRTH2

0.6 nM (Ki)

体外研究
(In Vitro)

CAY10471 Racemate (Compound 13) inhibits PGD2-induced inositol phosphate or cAMP formation, suppresses β-arrestin translocation with IC50s of 12 and 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

416.47

Formula

C21H21FN2O4S
CAS 号

844639-57-2
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 : 150 mg/mL (360.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4011 mL 12.0057 mL 24.0113 mL
5 mM 0.4802 mL 2.4011 mL 4.8023 mL
10 mM 0.2401 mL 1.2006 mL 2.4011 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 (6.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.00 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 (6.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.00 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 (6.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.00 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]. Ulven T, et al. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem. 2005 Feb 24;48(4):897-900.

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CAY10404

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。

CAY10404  纯度: 99.79%

CAY10404 是一种有效且高度选择性的环氧合酶 2 (COX-2) 抑制剂，IC50 为 1 nM，选择性指数 (SI；COX-1 IC50/COX-2 IC50) 为 >500000。CAY10404 是有效的 PKB/Akt 和 MAPK 信号通路抑制剂，可诱导非小细胞肺癌 (NSCLC) 细胞凋亡 (apoptosis)。CAY10404 是一种二芳基异恶唑，具有良好的止痛，抗炎和抗癌活性。

CAY10404

CAY10404 Chemical Structure

CAS No. : 340267-36-9

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 ￥1100 In-stock
5 mg ￥1000 In-stock
10 mg ￥1800 In-stock
25 mg ￥3800 In-stock
50 mg ￥6500 In-stock
100 mg ￥10500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CAY10404 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Pyroptosis Compound Library
  • Cytoskeleton Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[1][2][3].

IC50 & Target

COX-2

1 nM (IC50)

COX-1

>500 μM (IC50)

Akt

 

体外研究
(In Vitro)

CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500 µM)[1].
CAY10404 (10-100 µM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC50) of 60-100 µM[3].
CAY10404 (20-100 µM; for 3 days) induces apoptosis in NSCLC cells[3].
CAY10404 (80 µM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β[3].
CAY10404 (20, 50, 80, 100 µM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner[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.

Cell Viability Assay[3]

Cell Line: Non-small cell lung cancer (NSCLC) cells (H1703, H358, H460)
Concentration: 10-100 µM
Incubation Time: For 3 days
Result: Inhibited the growth of NSCLC cell lines in a concentration-dependent manner.

Apoptosis Analysis[3]

Cell Line: H460 cells
Concentration: 20, 50, 100 µM
Incubation Time: For 3 days
Result: Induced apoptosis.

Western Blot Analysis[3]

Cell Line: NSCLC cells (H358, H460)
Concentration: 80 µM
Incubation Time: For 3 days
Result: Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels.

体内研究
(In Vivo)

CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury[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 Model: Adult male C57Bl/6J mice weighing 24-30 g[2]
Dosage: 50 mg/kg
Administration: IP; daily; for 4 days
Result: Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α.
Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury.

分子量

367.34

Formula

C17H12F3NO3S
CAS 号

340267-36-9
运输条件

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

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (272.23 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7223 mL 13.6114 mL 27.2227 mL
5 mM 0.5445 mL 2.7223 mL 5.4445 mL
10 mM 0.2722 mL 1.3611 mL 2.7223 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 (stored under nitrogen)。-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 (6.81 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.81 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 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 (6.81 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.81 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
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.81 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]. A G Habeeb, et al. Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity. J Med Chem. 2001 Aug 30;44(18):2921-7.

    [2]. Joshua A Robertson, et al. The role of cyclooxygenase-2 in mechanical ventilation-induced lung injury. Am J Respir Cell Mol Biol. 2012 Sep;47(3):387-94.

    [3]. Yongseon Cho, et al. Effects of CAY10404 on the PKB/Akt and MAPK pathway and apoptosis in non-small cell lung cancer cells. Respirology. 2009 Aug;14(6):850-8.

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

CAY10505

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。

CAY10505  纯度: 99.75%

CAY10505 是一种有效的选择性 PI3Kγ 抑制剂，作用于神经元细胞，IC50 为 30 nM。

CAY10505

CAY10505 Chemical Structure

CAS No. : 1218777-13-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥500 In-stock
10 mg ￥420 In-stock
25 mg ￥750 In-stock
50 mg ￥1300 In-stock
100 mg ￥2100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CAY10505 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.

IC50 & Target[1]

PI3Kγ

30 nM (IC50, Neurons)

体外研究
(In Vitro)

A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC50=30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons[1]. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is tested on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analysed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, tested at 10 μM)[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)

Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly increases serum nitrite and (or) nitrate concentrations in hypertensive rats. Acetylcholine (ACh) and Sodium nitroprusside (SNP) produce endothelium-dependent and-independent relaxation in isolated rat aortic ring precontracted with Phenylephrine (3 μM), in a dose dependent manner. Administration of CAY10505 (0.6 mg/kg,p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly prevents hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation. Deoxycorticosterone acetate salt (DOCA, 40 mg/kg, s.c.) induced hypertension markedly attenuates acetylcholine-induced endothelium-dependent relaxation, but does not affect SNP-induced endotheliumindependent relaxation[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.
分子量

289.28

Formula

C14H8FNO3S
CAS 号

1218777-13-9
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 : ≥ 34 mg/mL (117.53 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 3.4569 mL 17.2843 mL 34.5686 mL
5 mM 0.6914 mL 3.4569 mL 6.9137 mL
10 mM 0.3457 mL 1.7284 mL 3.4569 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。
参考文献

  • [1]. Sun YY, Lin SH et al. Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. 2013 Jul 19;8(7):e69019.

    [2]. Tyagi S. Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats. Can J Physiol Pharmacol. 2012 Jul, 90(7), 881-5.

    [3]. Hofmann C, et al. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform. Br J Haematol. 2014 Aug;166(4):529-39.

    [4]. Jingyi Wang, et al. MiR-1976 Knockdown Promotes Epithelial-Mesenchymal Transition and Cancer Stem Cell Properties Inducing Triple-Negative Breast Cancer Metastasis. Cell Death Dis. 2020 Jul 3;11(7):500.

Cell Assay
[2]

Up to 5×104 multiple myeloma (MM) cells/100 μL of medium per well are seeded in 96-well-plates. Primary MM cells are always seeded into wells containing primary bone marrow stromal cells. Drugs (e.g., CAY10505) are dissolved in either DMSO or acidified ethanol (in the case of melphalan) and kept as frozen stock solutions of 10-50 mM. Working dilutions in fullmedium are always freshly prepared. In the case of Bortezomib small volumes of single-thaw stock solution aliquots are prepared. Drug dilutions (e.g., CAY10505, 2.5, 5, 7.5 and 10 μM) are added to MM cells as 100 μL of 2× the final concentration per well for single-drug treatments, and in appropriate volumes of higher concentrations for drug combinations. Solvent controls are always included[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
[3]

Rats[3]
Wistar albino rats (180-240 g) of either sex are employed in the present study. For each group, the number of rats used (n) is 6. Group I (normal control): Rats are maintained on a diet of normal chow with drinking water. Group II (hypertensive control): Rats are unilaterally nephrectomized (uninephrectomised) and DOCA (40 mg/kg) is administered by subcutaneous injection (s.c.) twice weekly for 6 weeks, and then the untreated drinking water is replaced with a 1% NaCl solution. Group III (hypertensive rats): Rats are treated with CAY10505 (0.6 mg/kg, per os (p.o)) for 1 week after 5 weeks of treatment with DOCA. Group IV (hypertensive rats): Rats are treated with Losartan (25 mg/kg, p.o.) for 1 week after 5 weeks of treatment with DOCA. Group V (hypertensive rats): Rats are treated with Atorvastatin (30 mg/kg, p.o.) for 1 week after 5 weeks of treatment with DOCA.

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]. Sun YY, Lin SH et al. Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. 2013 Jul 19;8(7):e69019.

    [2]. Tyagi S. Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats. Can J Physiol Pharmacol. 2012 Jul, 90(7), 881-5.

    [3]. Hofmann C, et al. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform. Br J Haematol. 2014 Aug;166(4):529-39.

    [4]. Jingyi Wang, et al. MiR-1976 Knockdown Promotes Epithelial-Mesenchymal Transition and Cancer Stem Cell Properties Inducing Triple-Negative Breast Cancer Metastasis. Cell Death Dis. 2020 Jul 3;11(7):500.

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

CAY10444(Synonyms: BML-241)

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。

CAY10444 (Synonyms: BML-241)

CAY10444 (BML-241) 是一种 sphingosine-1-phosphate 3 (S1P3) 拮抗剂。CAY10444 在表达 S1P3 受体的 HeLa 细胞中抑制 37% S1P 诱导的 Ca2+ 增加。

CAY10444(Synonyms: BML-241)

CAY10444 Chemical Structure

CAS No. : 298186-80-8

规格 是否有货
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250 mg   询价  
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生物活性

CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors[1].

IC50 & Target[1]

S1PR3

 

体外研究
(In Vitro)

BML-241 inhibits increases in intracellular Ca2+ concentration via P2 receptor or α1A-adrenoceptor stimulation and α1A-adrenoceptor-mediated contraction of rat mesenteric artery, while it does not affect S1P3-mediated decrease of Forskolin-induced cyclic AMP accumulation[1].

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

287.46

Formula

C15H29NO2S
CAS 号

298186-80-8
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]. Salvatore Salomone, et al. Selectivity and specificity of sphingosine-1-phosphate receptor ligands: caveats and critical thinking in characterizing receptor-mediated effects. Front Pharmacol. 2011 Feb 22;2:9.

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CAY10444(Synonyms: BML-241)

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。

CAY10444 (Synonyms: BML-241)

CAY10444 (BML-241) 是一种 sphingosine-1-phosphate 3 (S1P3) 拮抗剂。CAY10444 在表达 S1P3 受体的 HeLa 细胞中抑制 37% S1P 诱导的 Ca2+ 增加。

CAY10444(Synonyms: BML-241)

CAY10444 Chemical Structure

CAS No. : 298186-80-8

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

CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors[1].

IC50 & Target[1]

S1PR3

 

体外研究
(In Vitro)

BML-241 inhibits increases in intracellular Ca2+ concentration via P2 receptor or α1A-adrenoceptor stimulation and α1A-adrenoceptor-mediated contraction of rat mesenteric artery, while it does not affect S1P3-mediated decrease of Forskolin-induced cyclic AMP accumulation[1].

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

287.46

Formula

C15H29NO2S
CAS 号

298186-80-8
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]. Salvatore Salomone, et al. Selectivity and specificity of sphingosine-1-phosphate receptor ligands: caveats and critical thinking in characterizing receptor-mediated effects. Front Pharmacol. 2011 Feb 22;2:9.

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

CAY10444(Synonyms: BML-241)

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。

CAY10444 (Synonyms: BML-241)

CAY10444 (BML-241) 是一种 sphingosine-1-phosphate 3 (S1P3) 拮抗剂。CAY10444 在表达 S1P3 受体的 HeLa 细胞中抑制 37% S1P 诱导的 Ca2+ 增加。

CAY10444(Synonyms: BML-241)

CAY10444 Chemical Structure

CAS No. : 298186-80-8

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

CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors[1].

IC50 & Target[1]

S1PR3

 

体外研究
(In Vitro)

BML-241 inhibits increases in intracellular Ca2+ concentration via P2 receptor or α1A-adrenoceptor stimulation and α1A-adrenoceptor-mediated contraction of rat mesenteric artery, while it does not affect S1P3-mediated decrease of Forskolin-induced cyclic AMP accumulation[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

287.46

Formula

C15H29NO2S
CAS 号

298186-80-8
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]. Salvatore Salomone, et al. Selectivity and specificity of sphingosine-1-phosphate receptor ligands: caveats and critical thinking in characterizing receptor-mediated effects. Front Pharmacol. 2011 Feb 22;2:9.

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

CAY10621(Synonyms: SKI 5C)

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。

CAY10621 (Synonyms: SKI 5C)

CAY10621 (SKI 5C; Compound 5c) 是一种特异性的鞘氨醇激酶 1 (SPHK1) 抑制剂，IC50 为 3.3 μM。CAY10621 对细胞具有低毒性。CAY10621 具有抗癌肿瘤研究的潜力。

CAY10621(Synonyms: SKI 5C)

CAY10621 Chemical Structure

CAS No. : 120005-55-2

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

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生物活性

CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research[1].

分子量

435.64

Formula

C26H45NO4
CAS 号

120005-55-2
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]. Lingkai Wong, et al. Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases. J Med Chem. 2009 Jun 25;52(12):3618-26.

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

CAY10621(Synonyms: SKI 5C)

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。

CAY10621 (Synonyms: SKI 5C)

CAY10621 (SKI 5C; Compound 5c) 是一种特异性的鞘氨醇激酶 1 (SPHK1) 抑制剂，IC50 为 3.3 μM。CAY10621 对细胞具有低毒性。CAY10621 具有抗癌肿瘤研究的潜力。

CAY10621(Synonyms: SKI 5C)

CAY10621 Chemical Structure

CAS No. : 120005-55-2

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

CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research[1].

分子量

435.64

Formula

C26H45NO4
CAS 号

120005-55-2
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]. Lingkai Wong, et al. Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases. J Med Chem. 2009 Jun 25;52(12):3618-26.

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

CAY10621(Synonyms: SKI 5C)

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。

CAY10621 (Synonyms: SKI 5C)

CAY10621 (SKI 5C; Compound 5c) 是一种特异性的鞘氨醇激酶 1 (SPHK1) 抑制剂，IC50 为 3.3 μM。CAY10621 对细胞具有低毒性。CAY10621 具有抗癌肿瘤研究的潜力。

CAY10621(Synonyms: SKI 5C)

CAY10621 Chemical Structure

CAS No. : 120005-55-2

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

CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research[1].

分子量

435.64

Formula

C26H45NO4
CAS 号

120005-55-2
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]. Lingkai Wong, et al. Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases. J Med Chem. 2009 Jun 25;52(12):3618-26.

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

CAY10526

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。

CAY10526 

CAY10526 是特异性的微粒体前列腺素E2合成酶 1 (mPGES1)抑制剂。 CAY10526 通过选择性调节 mPGES1 表达抑制 PGE2 的产生，但不影响 COX-2。CAY10526 在黑色素瘤移植模型中抑制肿瘤生长并增加细胞凋亡。CAY10526 降低 BCL-2 和 BCL-XL (抗凋亡) 蛋白水平并增加 BAX 和 BAK (促凋亡) 以及切割的 caspase 3 水平。CAY10526 在三种表达 mPGES1的黑色素瘤细胞系中抑制细胞活力 (IC50<

CAY10526

CAY10526 Chemical Structure

CAS No. : 938069-71-7

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

CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μm) in three melanoma cell lines expressing mpges1[1].

分子量

311.15

Formula

C12H7BrO3S
CAS 号

938069-71-7
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]. Sun-Hee Kim, et al. Microsomal PGE2 synthase-1 regulates melanoma cell survival and associates with melanoma disease progression. Pigment Cell Melanoma Res. 2016 May;29(3):297-308.

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

CAY10526

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。

CAY10526 

CAY10526 是特异性的微粒体前列腺素E2合成酶 1 (mPGES1)抑制剂。 CAY10526 通过选择性调节 mPGES1 表达抑制 PGE2 的产生，但不影响 COX-2。CAY10526 在黑色素瘤移植模型中抑制肿瘤生长并增加细胞凋亡。CAY10526 降低 BCL-2 和 BCL-XL (抗凋亡) 蛋白水平并增加 BAX 和 BAK (促凋亡) 以及切割的 caspase 3 水平。CAY10526 在三种表达 mPGES1的黑色素瘤细胞系中抑制细胞活力 (IC50<

CAY10526

CAY10526 Chemical Structure

CAS No. : 938069-71-7

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

CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μm) in three melanoma cell lines expressing mpges1[1].

分子量

311.15

Formula

C12H7BrO3S
CAS 号

938069-71-7
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]. Sun-Hee Kim, et al. Microsomal PGE2 synthase-1 regulates melanoma cell survival and associates with melanoma disease progression. Pigment Cell Melanoma Res. 2016 May;29(3):297-308.

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

CAY10526

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。

CAY10526 

CAY10526 是特异性的微粒体前列腺素E2合成酶 1 (mPGES1)抑制剂。 CAY10526 通过选择性调节 mPGES1 表达抑制 PGE2 的产生，但不影响 COX-2。CAY10526 在黑色素瘤移植模型中抑制肿瘤生长并增加细胞凋亡。CAY10526 降低 BCL-2 和 BCL-XL (抗凋亡) 蛋白水平并增加 BAX 和 BAK (促凋亡) 以及切割的 caspase 3 水平。CAY10526 在三种表达 mPGES1的黑色素瘤细胞系中抑制细胞活力 (IC50<

CAY10526

CAY10526 Chemical Structure

CAS No. : 938069-71-7

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

CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μm) in three melanoma cell lines expressing mpges1[1].

分子量

311.15

Formula

C12H7BrO3S
CAS 号

938069-71-7
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]. Sun-Hee Kim, et al. Microsomal PGE2 synthase-1 regulates melanoma cell survival and associates with melanoma disease progression. Pigment Cell Melanoma Res. 2016 May;29(3):297-308.

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

CAY10594

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。

CAY10594 

CAY10594 是一种有效的磷脂酶 D2 (PLD2) 抑制剂(体外 IC50=140 nM，细胞 IC50=110 nM)。CAY10594 在体外高度抑制乳腺癌细胞的侵袭性迁移，并通过调节磷酸化 GSK-3β/JNK 轴改善扑热息痛诱导的急性肝损伤。

CAY10594

CAY10594 Chemical Structure

CAS No. : 1130067-34-3

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

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生物活性

CAY10594 is a potent phospholipase D2 (PLD2) inhibitor both in vitro (IC50=140 nM) and in cells (IC50=110 nM)[1]. CAY10594 strongly inhibits the invasive migration of breast cancer cells in vitro and ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis[2].

分子量

428.53

Formula

C26H28N4O2
CAS 号

1130067-34-3
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]. Scott, S.A., Selvy, P.E., Buck, J.R., et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness

    [2]. Lee SK, et al. A phospholipase D2 inhibitor, CAY10594, ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis. Sci Rep. 2019 May 10;9(1):7242.

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VU0155069(Synonyms: CAY10593)

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。

VU0155069 (Synonyms: CAY10593)

VU0155069 (CAY10593)，化合物 69 是一种选择性磷脂酶 D1 (PLD1) 抑制剂，IC50 值为 46 nM。VU0155069 (CAY10593) 在 transwell 测定中强烈抑制几种癌细胞系的侵袭性迁移。

VU0155069(Synonyms: CAY10593)

VU0155069 Chemical Structure

CAS No. : 1130067-06-9

规格 是否有货
5 mg 询价

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生物活性

VU0155069 (CAY10593), compound 69, is a selective phospholipase D1 (PLD1) inhibitor with an IC50 value of 46 nM in vitro[1]. VU0155069 (CAY10593) strongly inhibits the invasive migration of several cancer cell lines in transwell assays[2].

IC50 & Target

PLD1

46 nM (IC50)

PLD2

933 nM (IC50)

分子量

462.97

Formula

C26H27ClN4O2
CAS 号

1130067-06-9
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]. Scott SA, et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol. 2009 Feb;5(2):108-17.

    [2]. 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 Apr 1;19(7):1916-20.

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

CAY10603(Synonyms: BML-281)

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。

CAY10603 (Synonyms: BML-281) 纯度: 99.62%

CAY10603 (BML-281) 是一种有效的，选择性的 HDAC6 抑制剂，IC50 值为 2 pM；CAY10603 (BML-281) 同时可抑制 HDAC1，HDAC2，HDAC3，HDAC8 和 HDAC10 的活性，IC50 值分别为 271，252，0.42，6851，90.7 nM。

CAY10603(Synonyms: BML-281)

CAY10603 Chemical Structure

CAS No. : 1045792-66-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1081 In-stock
5 mg ￥1100 In-stock
10 mg ￥1800 In-stock
25 mg ￥3500 In-stock
50 mg ￥5500 In-stock
100 mg ￥8000 In-stock
200 mg   询价  
500 mg   询价  

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CAY10603 相关产品

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  • Anti-Liver Cancer Compound Library

生物活性

CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.

IC50 & Target[1]

HDAC6

0.002 nM (IC50)

HDAC3

0.42 nM (IC50)

HDAC10

90.7 nM (IC50)

HDAC2

252 nM (IC50)

HDAC1

271 nM (IC50)

HDAC8

6851 nM (IC50)

体外研究
(In Vitro)

CAY10603 (Compound 7) shows potent inhibitory activities against pancreatic cancer cell lines, with IC50s of 1, 0.3, 0.1, 0.1, 0.6, <1, 0.5 μM for BxPC-3, HupT3, Mia Paca-2, Panc 04.03, SU.86.86, HMEC, HPDE6c7, respectively. CAY10603 (100 nM, 200-300 nM) is active against both the Mia Paca-2 and Panc04.03 cell lines[1]. CAY10603 inhibits HDAC6 deacetylase activity, and supresses the proliferation of lung adenocarcinoma cells. CAY10603 also induces apoptosis of lung adenocarcinoma cells. Furthermore, CAY10603 synergizes with gefitinib to induce apoptosis in lung adenocarcinoma cell lines, partly through the destabilization of EGFR and inactivation of the EGFR pathway[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

446.50

Formula

C22H30N4O6
CAS 号

1045792-66-2
运输条件

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

DMSO : ≥ 50 mg/mL (111.98 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 2.2396 mL 11.1982 mL 22.3964 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 mL
10 mM 0.2240 mL 1.1198 mL 2.2396 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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 (5.60 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.60 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]. Kozikowski AP, et al. Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. J Med Chem. 2008 Aug 14;51(15):4370-3.

    [2]. Wang Z, et al. HDAC6 promotes cell proliferation and confers resistance to gefitinib in lung adenocarcinoma. Oncol Rep. 2016 Jul;36(1):589-97.
Kinase Assay
[1]

Purified HDACs are incubated with 1 mm carboxyfluorescein (FAM)-labeled acetylated peptide substrate and test compound for 17 h at 25°C in HDAC assay buffer containing 100 mm HEPES (pH 7.5), 25 mm KCl, 0.1% BSA, and 0.01% Triton X-100. Reactions are terminated by the addition of buffer containing 0.078% SDS for a final SDS concentration of 0.05%. Substrate and product are separated electrophoretically using a Caliper LabChip 3000 system with blue laser excitation and green fluorescence detection (CCD2). The fluorescence intensity in the substrate and product peaks is determined using the Well Analyzer software on the Caliper system. The reactions are performed in duplicate for each sample. IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the XLFit 4-Parameter Logistic Model (sigmoidal dose-response model): ((A+ ((B_A)/1+((C/x)D)))), in which x is compound concentration, A and B are respectively the estimated minimum and maximum of percent inhibition, C is the inflection point, and D is the Hill slope of the sigmoidal curve.

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 pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 are obtained from ATCC and are grown in medium (DMEM or RPMI) containing 10% fetal calf serum and l-glutamine. Pancreatic cancer cells are plated out in duplicate into 6 wells of a 96-well microtiter plate at 2.5-4P103 cells per well. Four hours post plating, individual wells are treated with diluent (DMSO) or varying concentrations of SAHA or the indicated HDACIs from a concentration of 1 nm to 50 mm. Cytotoxicity is measured at time “0”, and 72 h post treatment using the colorimetric MTT assay. The IC50 values are calculated using XLfit.

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]. Kozikowski AP, et al. Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. J Med Chem. 2008 Aug 14;51(15):4370-3.

    [2]. Wang Z, et al. HDAC6 promotes cell proliferation and confers resistance to gefitinib in lung adenocarcinoma. Oncol Rep. 2016 Jul;36(1):589-97.

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

GPP78(Synonyms: CAY10618)

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。

GPP78 (Synonyms: CAY10618) 纯度: ≥99.0%

GPP78 (CAY10618) 是一种有效的烟酰胺磷酸核糖转移酶 (Nampt) 抑制剂，对 NAD 消耗的 IC50 为 3 nM。GPP78 通过诱导自噬对神经母细胞瘤细胞 SH-SY5Y 具有毒性，IC50 为 3.8 nM。GPP78 具有抗癌和抗炎作用。

GPP78(Synonyms: CAY10618)

GPP78 Chemical Structure

CAS No. : 1202580-59-3

规格 价格 是否有货 数量
5 mg (11.38 mM * 1 mL in Methanol) ￥5400 In-stock

* Please select Quantity before adding items.

生物活性

GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects[1][2].

IC50 & Target

Nampt[1];
Autophagy[1]
体外研究
(In Vitro)

GPP78 (Compound 8; 10 nM; 24-40 hours; SH-SY5Y cells) treatment with cells, punctate staining of LC3-II and the formation of autophagolysosomes are observable. LC3-II is membrane-bound and is present in autophagosomes[1].
GPP78 (Compound 8) inhibits the growth of most cell lines tested, with nanomolar potency (GI50) in cell lines derived from leukemia, lung, CNS, colon, melanoma, ovarian, renal, and prostate cancers. GPP78 appears truly cytotoxic in melanoma cell lines, while in the others it is mainly cytostatic[1].

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

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 10 nM
Incubation Time: 24 hours, 40 hours
Result: Punctate staining of LC3-II and the formation of autophagolysosomes were observable.

体内研究
(In Vivo)

GPP78 (10 mg/kg; intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days; male adult CD1 mice) treatment reduces the severity of spinal cord trauma in SCI mice[2].

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

Animal Model: Male adult CD1 mice (25-30 g) with spinal cord injury (SCI)[2]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days
Result: Significantly reduced the demyelination associated with SCI. And significantly ameliorated the functional deficits induced by SCI.

分子量

439.55

Formula

C27H29N5O
CAS 号

1202580-59-3
运输条件

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

Solution, -20°C, 2 years
参考文献

  • [1]. Colombano G, et al. A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistry. J Med Chem. 2010 Jan 28;53(2):616-23.

    [2]. Esposito E, et al. The NAMPT inhibitor FK866 reverts the damage in spinal cord injury. J Neuroinflammation. 2012 Apr 10;9:66.

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

CAY10566

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。

CAY10566  纯度: 99.73%

CAY10566 是一种有效的，生物口服可利用的，选择性的硬脂酰辅酶 A 去饱和酶 1 (SCD1) 抑制剂，在小鼠和人酶测定中 IC50 分别为 4.5 和 26 nM。CAY10566 具有优异的细胞活性，可阻断 HepG2 细胞中饱和长链脂肪酸-CoAs (LCFA-CoAs) 向单不饱和 LCFA-CoAs 的转化 (IC50=7.9 nM 或 6.8 nM)。

CAY10566

CAY10566 Chemical Structure

CAS No. : 944808-88-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2090 In-stock
1 mg ￥600 In-stock
5 mg ￥1900 In-stock
10 mg ￥3600 In-stock
25 mg ￥7900 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

CAY10566 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Obesity Compound Library
  • Lipid Metabolism Compound Library

生物活性

CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM)[1][2].

IC50 & Target

IC50: 4.5 nM (SCD1 in mouse), 26 nM (SCD1 in human)[2]
体外研究
(In Vitro)

CAY10566 (0.0001-10 μM; 24 hours) concentration-dependently decreases Swiss 3T3 cell proliferation[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.

Cell Proliferation Assay[3]

Cell Line: Swiss 3T3 cells
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 hours
Result: Swiss 3T3 cell proliferation was concentration-dependently decreased.

体内研究
(In Vivo)

After establishment of palpable tumors, the mice are treated with vehicle or SCD1 inhibitor (2.5 mg/kg CAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on the Ras-driven tumors, with the mean tumor volume at day 13 or 14 post therapy, relative to untreated tumors, 0.5±0.04 and 0.67±0.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t test)[4].

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

389.81

Formula

C18H17ClFN5O2
CAS 号

944808-88-2
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 (64.13 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5654 mL 12.8268 mL 25.6535 mL
5 mM 0.5131 mL 2.5654 mL 5.1307 mL
10 mM 0.2565 mL 1.2827 mL 2.5654 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: ≥ 2.5 mg/mL (6.41 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.41 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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.41 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。

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.34 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 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

*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]. Masuda M, et al. Activating transcription factor 4 regulates stearate-induced vascular calcification. J Lipid Res. 2012 Aug;53(8):1543-52.

    [2]. Liu G, et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem. 2007 Jun 28;50(13):3086-100.

    [3]. Koeberle A, et al. Palmitoleate is a mitogen, formed upon stimulation with growth factors, and converted to palmitoleoyl-phosphatidylinositol. J Biol Chem. 2012 Aug 3;287(32):27244-54.

    [4]. Kamphorst JJ, et al. Hypoxic and Ras-transformed cells support growth by scavenging unsaturated fatty acids from lysophospholipids. Proc Natl Acad Sci U S A. 2013 May 28;110(22):8882-7.

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

Santacruzamate A(Synonyms: CAY-10683)

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。

Santacruzamate A (Synonyms: CAY-10683) 纯度: 99.32%

Santacruzamate A (CAY-10683) 是一种高效的选择性 HDAC2 抑制剂，IC50 为 119 pM。

Santacruzamate A(Synonyms: CAY-10683)

Santacruzamate A Chemical Structure

CAS No. : 1477949-42-0

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 ￥605 In-stock
5 mg ￥550 In-stock
10 mg ￥650 In-stock
50 mg ￥2500 In-stock
100 mg ￥4000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Santacruzamate A 相关产品

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  • Alkaloids Library
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  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Microbial Metabolite Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

Santacruzamate A (CAY-10683) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM[1].

IC50 & Target[1]

HDAC2

119 pM (IC50)

HDAC6

434 nM (IC50)

分子量

278.35

Formula

C15H22N2O3
CAS 号

1477949-42-0
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 : ≥ 100 mg/mL (359.26 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 3.5926 mL 17.9630 mL 35.9260 mL
5 mM 0.7185 mL 3.5926 mL 7.1852 mL
10 mM 0.3593 mL 1.7963 mL 3.5926 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 (8.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.98 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 (8.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.98 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 (8.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.98 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]. Pavlik CM,et al. Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp. J Nat Prod. 2013 Nov 22;76(11):2026-33.

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