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CLK1-IN-1

    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 2123491-32-5
  • 分子式: C24H16FN5O
  • 分子量: 409.42
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货号 (SKU) 包装规格 是否现货 价格 数量
C656461-1ml
1ml 期货 Stock Image

基本描述

别名 CLK1-输入-1
规格或纯度 10mM in DMSO
英文名称 CLK1-IN-1
生化机理 CLK1-IN-1 是一种强效的 Cdc2 样激酶 1(CLK1)选择性抑制剂,其 IC 50 为 2 nM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 ( CLK1 ) inhibitor, with an IC 50 of 2 nM.

In Vitro

CLK1 is the most potently inhibited kinase (IC 50 : 2 nM). In addition to CLK1, only two kinases have an IC 50 value less than 100 nM, namely CLK2 (IC 50 : 31 nM) and CLK4 (IC 50 : 8 nM), DYRK1A is the strongest off-target. The ability of CLK1-IN-1 to induce autophagy in BNL CL.2 and SKOV-3 (human ovarian cancer cell line) cells is also examined. The effects of CLK1-IN-1 on yellow LC3 puncta also displays obvious dose dependency, and a dose of 10 μM shows the best performance. In addition, in CLK1-IN-1-treated cells, the number of red LC3 puncta (mRFP signals only35) increases compared with that of DMSO-treated cells, indicating the formation of autolysosomes. Importantly, CLK1-IN-1 stimulats the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate an induction of autophagic flux by CLK1-IN-1. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

APAP exposure results in severe liver injury, and treatment with CLK1-IN-1 (ip, 30 mg/kg) imparts a significant hepatoprotective effect. The results show that treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:CLK1 2 nM (IC 50 )

关联靶点(人)

CLK1 Tchem 双特异性蛋白激酶 CLK1(Dual specificity protein kinase CLK1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CLK4 Tchem 双特异性蛋白激酶 CLK4(Dual specificity protein kinase CLK4) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES C[C@@H](C1=CC=C(C=C1)F)N2C3=C4C=C(C=CC4=NC=C3N=N2)C5=CC6=C(C=C5)OC=N6
PubChem CID 129318964
分子量 409.42

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