RGB-286147

RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with 50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

CDK1/cyclinB:48 nM (IC50)

CDK2/E:15 nM (IC50)

CDK4/D1:839 nM (IC50)

cdk6/cyclin D3:232 nM (IC50)

RGB-286147（50-100 nM；24-48 小时）在 G1 期诱导细胞周期停滞，显着抑制 DNA 复制，并诱导 HCT116 细胞凋亡[1]。 RGB-286147（100 nM；48 小时）导致 HCT116 细胞中 PARP 的蛋白水解裂解[1]。 RGB-286147（24-72 小时）在 HCT116 细胞中表现出有效且不可逆的细胞杀伤活性。RGB-286147 抑制集落形成的 IC50 值为 57 nM[1]。 RGB-286147（48 小时）表现出广泛的抗肿瘤活性，对于 60 种致瘤细胞系，平均 GI50 值 <10 nM。并且还抑制非循环 HCT116 细胞的生长，IC50 值为 40 nM[1]。 Cell Cycle Analysis[1] Cell Line: HCT116 cells Concentration: 50 nM and 100 nM Incubation Time: 24 or 48 hr Result: Caused a marked inhibition of DNA replication and induced cell cycle arrest. Western Blot Analysis[1] Cell Line: HCT116 cells Concentration: 100 nM Incubation Time: 48 hr Result: Resulted in proteolytic cleavage of PARP.

[1]. Maureen Caligiuri, et al. A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. Chem Biol. 2005 Oct;12(10):1103-15.