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BRD4 degrader AT1
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。
BRD4 degrader AT1图片
CAS NO:2098836-45-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
BRD4degraderAT1是基于PROTAC技术的一种高度选择性的Brd4降解剂,在细胞中对Brd4BD2的Kd值为44nM。
Cas No.2098836-45-2
Canonical SMILESCC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@@H](CC(NCCCCCCSC(C)(C)[C@H](NC(C)=O)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)C7=NN=C(C)N27
分子式C48H58ClN9O5S3
分子量972.68
溶解度DMSO : 100 mg/mL (102.81 mM)
储存条件Store at -20°C
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

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

BRD4 degrader AT1 is a highly selective Brd4 degrader, with a Kd of 44 nM, for Brd4BD2 in cells. BRD4 degrader AT1 also shows Kds of 38.8 nM for a mutant Brd4BD2 (QVK), 111 ± 14 nM for Brd2BD1, 94 ± 9 nM for Brd2BD2, 35 ± 3 nM for Brd3BD1, 39 ± 8 nM for Brd3BD2, 75 ± 23 nM for Brd4BD1 and 35 ± 4 nM for a Brd2BD1 mutant (KEA). BRD4 degrader AT1 (1-3 μM) causes remarkable Brd4-selective depletion and has no or little activity against Brd2 and Brd3[1].

[1]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521.