Chk
CSK-homologous kinase (CHK), a protein kinase that displays significant sequence similarity with CSK. Depending on its structural features and the origins of the cDNA libraries, CHK was also named Hyl, BatK, Matk, Ctk and Ntk. Both CSK and CHK are cytosolic protein tyrosine kinases. Membrane translocation of CHK is mainly mediated by binding to membrane proteins and signaling adaptor proteins via their SH2, SH3 and/or kinase domains CHK is recruited to the plasma membrane by binding to membrane proteins ErbB2, c-Kit, and TrkA via its SH2 domain. Deletion of the SH3 domain abolishes the abilities of CHK to anchor to the plasma membrane to inhibit Lyn, and to suppress cell spreading. Mutation of Ser-78 in the SH3 –SH2 connector of CHK resulted in a significant loss of activity. CHK may perform unique functions in the nucleus and these functions are related to the ability of CHK to suppress myeloid cell growth.
References
1.Chong YP,et al. Growth Factors. 2005 Sep;23(3):233-44.
References
1.Chong YP,et al. Growth Factors. 2005 Sep;23(3):233-44.
Angiogenesis
Chk
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4-Demethyldeoxypodophyllotoxin
产品货号 : M37321
cas no: 3590-93-0
4-Demethyldeoxypodophyllotoxin 是一种芳基四氢萘木酚素,存在于 Podophyllum peltatum 中。 -
PHI-101
产品货号 : M37298
cas no: 2127107-15-5
PHI-101 是一种口服有效的 FLT3 抑制剂,可克服对多种耐药突变的耐药性。PHI-101 有效抑制 FLT3 单激活突变 (ITD 或 TKD 突变体),并对 FLT3 双 (ITD/D835Y 或 ITD/F691L) 和三 (ITD/D835Y/F691L) 耐药突变 具有抑制活性。PHI-101 有望应用于复发或难治性急性髓系白血病 (AML) 的研究。 -
Monalizumab
产品货号 : M36667
cas no: 1228763-95-8
Monalizumab (IPH2201) 是一种靶向自然杀伤细胞群 2A (NKG2A) 的免疫检查点抑制剂。Monalizumab 是一种人源化抗 NKG2A 的单克隆抗体,可增加 IFN-γ 产生,从而促进自然杀伤细胞功能。Monalizumab 可用于头颈部鳞状细胞癌 (HNSCC) 的研究。 -
Tuvusertib
产品货号 : M32792
cas no: 1613200-51-3
Tuvusertib (M1774; ATR inhibitor 1) 是一种选择性和具有口服活性的 ATR 抑制剂,Ki 值低于 1 μΜ,详细信息请参考专利 WO2015187451A1,化合物 I-l。 -
GDC0575 monohydrochloride
产品货号 : M27878
cas no: 1196504-54-7
GDC-0575 是一种有效的选择性细胞周期检查点激酶 1 (Chk1) 抑制剂,IC50 为 1.2 nM。 GDC-0575 特异性结合并抑制 Chk1;这可能导致肿瘤细胞绕过 S 期和 G2/M 期的 Chk1 依赖性细胞周期停滞,从而允许细胞在进入有丝分裂之前进行 DNA 修复。