货号:A118376 同义名: SC 204330;Pim-1 Kinase Inhibitor II
TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s > 20,000 nM).
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产品名称 | Pim1 ↓ ↑ | Pim2 ↓ ↑ | Pim3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SMI-4a |
++
Pim1, IC50: 17 nM |
99%+ | |||||||||||||||||
SGI-1776 free base |
++
Pim1, IC50: 7 nM |
+
Pim2, IC50: 363 nM |
+
Pim3, IC50: 69 nM |
FLT3 | 99+% | ||||||||||||||
AZD-1208 |
+++
Pim1, IC50: 0.4 nM |
+++
Pim2, IC50: 5 nM |
+++
Pim3, IC50: 1.9 nM |
98% | |||||||||||||||
CX-6258 HCl |
+++
Pim1, IC50: 5 nM |
+
Pim2, IC50: 25 nM |
++
Pim3, IC50: 16 nM |
98% | |||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Pim (provirus integration site for Moloney murine leukemia virus) family proteins are highly conserved serine/threonine kinases implicated in transcription, translation, cell cycle, survival, and drug resistance through the numerous targets. TCS PIM-1 1 is a Pim-1 inhibitor with IC50 value of 50nM (measured by Pim-1 kinase activity), lacking in vitro inhibitory activity toward related kinase Pim-2 and MEK1/2 (IC50 > 20μM)[1]. |
作用机制 | TCS PIM-1 1 can bound within the ATP-binding site of Pim-1, suggesting it as an ATP-competitive inhibitor.[1] |
Dose | Mice: 75 mg/kg[2] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.72mL 0.54mL 0.27mL |
13.62mL 2.72mL 1.36mL |
27.23mL 5.45mL 2.72mL |
CAS号 | 491871-58-0 |
分子式 | C18H11BrN2O2 |
分子量 | 367.196 |
别名 | SC 204330;Pim-1 Kinase Inhibitor II |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 105 mg/mL(285.95 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |