标签归档：quarterhydrate

iMDK quarterhydrate

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。

iMDK quarterhydrate  纯度: ≥99.0%

iMDK quarterhydrate 是一种有效的 PI3K 抑制剂，可抑制生长因子 MDK（也称为中期因子或 MK）。iMDK quarterhydrate 与 MEK 抑制剂协同抑制非小细胞肺癌 (NSCLC)，而不会伤害正常细胞和小鼠。

iMDK quarterhydrate

iMDK quarterhydrate Chemical Structure

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

iMDK quarterhydrate 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice[1].

体外研究
(In Vitro)

iMDK (50-500 nM) quarterhydrate suppressed AKT phosphorylation in a dose-dependent manner in H441 lung adenocarcinoma cells after treatment for 72 h. In contrast, iMDK quarterhydrate robustly increases p-ERK[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: H441 (lung adenocarcinoma; KRASG12V), H2009 (non-small cell carcinoma; KRASG12A), A549 (lung carcinoma; KRASG12S) and H520 (lung squamous cell carcinoma; KRASWT)
Concentration: iMDK (2.5 μM) quarterhydrate and PD0325901 (0.5 μM) for H441 and H2009 cells
iMDK (0.125 μM) quarterhydrate and PD0325901 (0.25 μM) for H520 cells
iMDK (0.25 μM) quarterhydrate and PD0325901 (0.125 μM) for A549 cells
Incubation Time: 72 hours
Result: iMDK quarterhydrate alone did not inhibit cell viability of A549 cells, the combinatorial treatment of iMDK quarterhydrate with PD0325901 significantly inhibited that of A549 cells compared to the single treatment of PD0325901.

Western Blot Analysis[1]

Cell Line: H441 lung adenocarcinoma cells
Concentration: 0-500 nM
Incubation Time: 72 hours
Result: Suppressed AKT phosphorylation in a dose-dependent manner.
ERK1/2 phosphorylation was increased.

体内研究
(In Vivo)

The combination treatment of iMDK ( (9 mg/kg/day; intraperitoneally injected with 100 μl) and PD0325901 (5 mg/kg; orally administered) effectively reduced lung tumor growth in a xenograft mouse model[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 Model: female BALB/c nude mice (6 week old) bearing H441 human lung cancer xenografts[1]
Dosage: iMDK (9 mg/kg) quarterhydrate and PD0325901 (5 mg/kg)
Administration: Intraperitoneally injected with 100 μL iMDK everyday and/or orally
Result: Reduced significantly volume of the tumors derived from H441 lung adenocarcinoma cells after the combination treatment with iMDK quarterhydrate and PD0325901 compared to that of single compound in a xenograft mouse model.

分子量

380.91

Formula

C21H15FN2O3S
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 : 12.8 mg/mL (33.60 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6253 mL 13.1265 mL 26.2529 mL
5 mM 0.5251 mL 2.6253 mL 5.2506 mL
10 mM 0.2625 mL 1.3126 mL 2.6253 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]. Naomasa Ishida, et al. A novel PI3K inhibitor iMDK suppresses non-small cell lung Cancer cooperatively with A MEK inhibitor. Exp Cell Res. 2015 Jul 15;335(2):197-206.

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

SID 26681509 quarterhydrate

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。

SID 26681509 quarterhydrate  纯度: ≥97.0%

SID 26681509 quarterhydrate 是一种有效的，可逆的，竞争性的，选择性的人组织蛋白酶 L (human cathepsin L) 抑制剂，IC50 为 56 nM。SID 26681509 quarterhydrate 抑制 Plasmodium falciparum 的体外繁殖，并抑制 Leishmania major，IC50 分别为 15.4 μM 和 12.5 μM。SID 26681509 quarterhydrate 对组织蛋白酶 G 没有抑制活性。

SID 26681509 quarterhydrate

SID 26681509 quarterhydrate Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥7120 In-stock
1 mg ￥1950 In-stock
5 mg ￥5800 In-stock
10 mg ￥9800 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

生物活性

SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G[1].

IC50 & Target

IC50: 56 nM (Human cathepsin L), 0.5 μM (Cathepsin V), 15.4 μM (Plasmodium falciparum), 12.5 μM (Leishmania major)[1]
体外研究
(In Vitro)

After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent, demonstrating an IC50 of 1.0 nM. SID 26681509 is determined to be a slow-binding and slowly reversible competitive inhibitor. Through a transient kinetic analysis for single-step reversibility, inhibition rate constants are kon = 24,000 M-1s-1 and koff = 2.2 × 10-5 s-1 (Ki = 0.89 nM). Molecular docking studies are undertaken using the experimentally-derived X-ray crystal structure of papain/CLIK-148[1].
SID 26681509 inhibits papain and cathepsins B, K, S, and V with IC50 values determined after one hour ranging from 618 nM to 8.442 μM. SID 26681509 shows no inhibitory activity against the serine protease cathepsin G[1].
SID 26681509 inhibits cathepsin V activity with an IC50 value of 0.5 μM. SID 26681509 (1-30 μM) blocks high-mobility group box 1 (HMGB1)-induced TNF-α production dose dependently without altering cell viability[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)

SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models[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

544.16

Formula

C27H35N5O6S
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 : 27 mg/mL (49.62 mM; Need ultrasonic and warming)

Ethanol : 5 mg/mL (9.19 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8377 mL 9.1885 mL 18.3769 mL
5 mM 0.3675 mL 1.8377 mL 3.6754 mL
10 mM 0.1838 mL 0.9188 mL 1.8377 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: ≥ 1.67 mg/mL (3.07 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.07 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 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]. Shah PP, et al. Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L. Mol Pharmacol. 2008 Jul;74(1):34-41.

    [2]. Pribis JP, et al. The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88. Mol Med. 2015 Dec;21(1):749-757.

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