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KH CB19
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
KH CB19图片
CAS NO:1354037-26-5
包装:1mg
市场价:683元

产品介绍
KH CB19 是一种有效的 CLK（cdc2 样激酶）抑制剂（CLK1 IC50\u003d19.7 nM；CLK3 IC50\u003d530 nM）。
Cas No.1354037-26-5
化学名(E)-ethyl 3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate
Canonical SMILESClC1=C2N(C)C(C(OCC)=O)=C(/C(C#N)=C\N)C2=CC=C1Cl
分子式C15H13Cl2N3O2
分子量338.19
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

KH CB19 is a potent and selective inhibitor of CLK1 and CLK4 with IC50 values of 19.7 and 530 nM for CLK1 and CLK3, respectively [1] [2].

The cdc2-like kinases (CLKs) are dual specificity protein kinases that phosphorylate the serine- and arginine-rich (SR) proteins, which are involved in regulating the alternative pre-mRNA splicing process [1].

KH CB19 is a potent and selective inhibitor of CLK1 and CLK4. In endothelial cells, KH CB19 inhibited the phosphorylation of serine- and arginine-rich (SR) proteins stimulated by TNF-α and decreased the mRNA expression of tissue factor splice variants [1]. KH CB19 bound to the ATP binding site in CLK3 and CLK1. In enzyme kinetic assays, KH CB19 inhibited DYRK1A with IC50 value of 55.2 nM. In human microvascular endothelial cells (HMEC-1), KH-CB19 (10 μM) reduced the phosphorylation of SRp75, SRp55 and SRp20. However, in TNF-α stimulated HMEC-1, KH-CB19 (10 μM) inhibited the phosphorylation of SRp75, SRp55, SRp40, SC35, SF2/ASF and SRp20. In HMEC-1, KH CB19 (10 μM) significantly reduced the expression of the membrane bound full-length tissue factor (flTF) as well as the soluble asHTF in TNF-α-induced and TNF-α-non-induced cells [2].

References:
[1].  Grant SK, Lunney EA. Kinase inhibition that hinges on halogen bonds. Chem Biol, 2011, 18(1): 3-4.
[2].  Fedorov O, Huber K, Eisenreich A, et al. Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol, 2011, 18(1): 67-76.