BTX161 一种 ThalIDOmide 类似物,是一种有效的CKIα降解剂。BTX161 比 LenalIDOmide更好地介导人类 AML 细胞中 CKIα 的降解,并激活 DNA损伤反应 (DDR) 和 p53,同时稳定 p53 拮抗剂 Mdm2。
产品描述
BTX161, a Thalidomide analog, is a potent CKIα degrader. BTX161 mediates degradation of CKIα better than Lenalidomide in human AML cells and activates DNA damage response (DDR) and p53, while stabilizing the p53 antagonist MDM2 [1].
体外活性
BTX161 (25 μM; 4 hours; MV4-11 cells) upregulates all the Wnt targets including MYC and did not affect MDM2 mRNA expression [1]. BTX161 (10 μM; 6 hours; MV4-11 cells), on its own, augmented p53 and MDM2 protein expression, yet in combination with THZ1, and particularly with both THZ1 and CDK9, further augmented p53 and induced maximal caspase 3 activation [1].
Cas No.
2052301-24-1
分子式
C15H16N2O3
分子量
272.3
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years