chk1 in 2

CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).

GDC-0425 (RG-7602) 是一种可口服的、高选择性的 ChK1抑制剂。GDC-0425 可用于多种恶性肿瘤的研究。

Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes. Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID:21186793

Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物，可激活Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。它能够降低炎性因子水平，激活 NF-κB，抑制COX-2的表达，具有抗癌和抗炎作用。

Compound PROTAC-2, also known as PROTAC Chk1 degrader-1, is a potent degrader of Chk1, exhibiting a DC50 of 1.33 μM. It is utilized in cancer research [1].