Bioactivity | HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1]. |
Invitro | HEMTAC CDK4/6 degrader 1 (compound 26; 0.01-1 μM; 24 h) 在处理过的 B16F10 细胞中诱导 CDK4 和 CDK6 降解,DC50 值 (产生 50% 蛋白质的药物浓度 降解) 约为 26 和 19 nM,Dmax (最大降解百分比) 分别为 88% 和 92%[1]。HEMTAC CDK4/6 degrader 1 (0.01-100 μM; 72 h) 对多种人类癌细胞系具有抗增殖活性[1]。HEMTAC CDK4/6 degrader 1 (250 nM; 24 or 48 h) 以剂量依赖的方式诱导 B16F10 细胞发生凋亡,并使细胞周期停滞在 G0/G1 期[1]。 Cell Viability Assay[1] Cell Line: |
Name | HEMTAC CDK4/6 degrader 1 |
CAS | 2821803-61-4 |
Formula | C48H53ClN16O4 |
Molar Mass | 953.49 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |