常用名:dCBP-1
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].
分子量 1028.11
分子式 C51H63F2N11O10
CAS No. 2484739-25-3
存储
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度
DMSO: 50 mg/mL (48.63 mM)
PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来,从而“劫持”细胞的泛素-蛋白酶体系统(UPS)来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标(而不是抑制靶蛋白的酶活性),目前有许多努力将先前无效的抑制剂分子改造为 PROTACs,用作下一代药物。
产地:西安
用途:科研!
厂家:西安齐岳生物科技有限公司
温馨提示:仅用于科研,不能用于人体实验!
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