K145 hydrochloride

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。

K145 hydrochloride  纯度: 99.34%

K145 hydrochloride 是一种选择性的,具有底物竞争性和口服活性的 SphK2 抑制剂,IC50 为 4.3 µM,Ki 为 6.4 µM。K145 hydrochloride 对 SphK1 和其他蛋白激酶没有活性。K145 hydrochloride 可诱导细胞凋亡,并具有强大的抗肿瘤活性。

K145 hydrochloride

K145 hydrochloride Chemical Structure

CAS No. : 1449240-68-9

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 ¥726 In-stock
5 mg ¥660 In-stock
10 mg ¥1100 In-stock
50 mg ¥3950 In-stock
100 mg ¥7100 In-stock
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500 mg   询价  

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K145 hydrochloride 相关产品

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生物活性

K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity[1].

IC50 & Target

IC50: 4.3 µM (SphK2)[1]
Ki: 6.4 µM (SphK2)[1]

体外研究
(In Vitro)

K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner[1].
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells[1].
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt[1].
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels[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: U937 cells
Concentration: 0 µM, 4 µM, 6 µM, 8 µM, 10 µM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Significantly inhibited the growth of U937 cells in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: U937 cells
Concentration: 10 µM
Incubation Time: 24 hours
Result: Significantly induced apoptosis in U937 cells.

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 4 µM, 8 µM
Incubation Time: 3 hours
Result: Phosphorylated ERK and Akt were decreased.

体内研究
(In Vivo)

K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice[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: BALB/c-nu mice injected with U937 cells[1]
Dosage: 50 mg/kg
Administration: Oral gavage; daily; for 15 days
Result: Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.

分子量

384.92

Formula

C18H25ClN2O3S

CAS 号

1449240-68-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 126.7 mg/mL (329.16 mM; Need ultrasonic and warming)

DMSO : 50 mg/mL (129.90 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5979 mL 12.9897 mL 25.9794 mL
5 mM 0.5196 mL 2.5979 mL 5.1959 mL
10 mM 0.2598 mL 1.2990 mL 2.5979 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 (sealed storage, away from moisture)。-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: ≥ 0.83 mg/mL (2.16 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.16 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 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: ≥ 0.83 mg/mL (2.16 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.16 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 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: ≥ 0.83 mg/mL (2.16 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.16 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 8.3 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]. Liu K, et al. Biological characterization of 3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) as a selective sphingosine kinase-2 inhibitor and anticancer agent. PLoS One. 2013;8(2):e56471.

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