[CAS NO. 1950634-92-0]  dBET6

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PRODUCTS SPECIFICATIONS [1950634-92-0]

Catelog
SLK-S8762
Brand
Selleck
CAS
1950634-92-0

DESCRIPTION [1950634-92-0]

Overview

MDL-
Molecular Weight841.37
Molecular FormulaC42H45ClN8O7S
SMILESO=C(NCCCCCCCCNC(COC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.1885 mL5.9427 mL11.8854 mL
5 mM0.2377 mL1.1885 mL2.3771 mL
10 mM0.1189 mL0.5943 mL1.1885 mL
50 mM0.0238 mL0.1189 mL0.2377 mL

Description

dBET6 is a highly cell-permeable PROTAC degrader of with an IC50 of 14 nM for BRD4 binding. dBET6 also induces downregulation and .

Targets

BRD4 [1]
14 nM

In vitro

dBET6 is a highly cell-permeable degrader of BET bromodomains. It is potent in most cancer cell lines. dBET6 features highly increased cellular potency with evident degradation in the sub-nanomolar range. Treatment with 100 nM dBET6 leads to degradation of BRD4 after 1 hr, prompting subsequent downregulation of c-MYC and induction of apoptosis. dBET6 disrupts global productive transcription elongation. dBET6 treatment leads to a widespread decrease in steady-state mRNA levels, but observed an incommensurate impact on expression of members of the core regulatory circuitry of leukemogenic transcription factors. The collapse of the core transcriptional machinery prompted by BET degradation precedes a robust apoptotic response, of apparent translational significance.