dCBP-1 是基于Cereblon配体的p300/CBP的选择性双功能降解剂。dCBP-1可以有效的杀死多发性骨髓瘤细胞,并降低驱动 MYC 表达的致癌增强子活性。
产品描述
dCBP-1 is a chemical degrader of p300/CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300/CBP. Degradation of p300/CBP by dCBP-1 leads to effective multiple myeloma cell killing.
体外活性
Treatment of the human haploid cell line HAP1 for 6 h with dCBP-1 revealed almost complete loss of both CBP and p300 between 10 and 1,000 nM doses. A time course analysis with 250 nM dCBP-1 revealed almost complete degradation of p300/CBP within an hour of treatment[1]. dCBP-1 was also able to induce near-complete p300/CBP degradation across other multiple myeloma cell lines tested, including MM1R, KMS-12-BM, and KMS34[1].
Cas No.
2484739-25-3
分子式
C51H63F2N11O10
分子量
1028.11
储存和溶解度
DMSO:50 mg/mL (48.63 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years