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dCBP-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
dCBP-1图片
CAS NO:2484739-25-3
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
dCBP-1 是一种基于 PROTAC 的 p300/CBP 的有效且选择性的异双功能降解剂。dCBP-1 在杀死多发性骨髓瘤细胞方面非常有效,并降低了驱动 MYC 表达的致癌增强子活性。
Cas No.2484739-25-3
分子式C51H63F2N11O10
分子量1028.11
溶解度DMSO : 50 mg/mL (48.63 mM; ultrasonic and warming and heat to 80°C)
储存条件Store at -20°C, sealed storage, away from moisture and light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression[1].

dCBP-1 (10-1000 nM; 6 hours) treatment shows near-complete degradation of p300/CBP in MM1S cells. dCBP-1 is also able to induce near-complete p300/CBP degradation across other multiple myeloma cell lines tested, including MM1R, KMS-12-BM, and KMS34[1].Treatment of the human haploid cell line HAP1 for 6 h with dCBP-1 reveals almost complete loss of both CBP and p300 between 10 and 1000 nM doses. A time course analysis with 250 nM dCBP-1 revealed almost complete degradation of p300/CBP within an hour of treatment[1].

[1]. Raghu Vannam, et al. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell Chem Biol. 2020 Dec 31;S2451-9456(20)30513-4.