dBET1 ( dBET 1 )

Catalog No. M12725 CAS No. 1799711-21-9

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HPLC

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Product Name

dBET1
Note

Research use only, not for human use.
Brief Description

dBET1 is a proteolysis-targeting chimera (PROTAC) molecule that appendes a competitive antagonist of BET bromodomain (JQ1) to a phthalimide moiety to hijack the cereblon E3 ubiquitin ligase complex.
Description

dBET1 is a proteolysis-targeting chimera (PROTAC) molecule that appendes a competitive antagonist of BET bromodomain (JQ1) to a phthalimide moiety to hijack the cereblon E3 ubiquitin ligase complex; induces highly selective cereblon-dependent BET protein degradation in vitro (EC50=430 nM) and in vivo and delayed leukemia progression in mice.
Synonyms

dBET 1
Pathway

PROTACs
Target

PROTAC
Recptor

BET
Research Area

——
Indication

——

CAS Number

1799711-21-9
Formula Weight

785.27
Molecular Formula

C38H37ClN8O7S
Purity

>98% (HPLC)
Solubility

DMSO: 50 mg/mL; Water: Insoluble; Ethanol: 5 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )
SMILES

CC(N(C1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1)CCCCNC(COC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)=O
Chemical Name

(6S)-4-(4-chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

1. Winter GE, et al. Science. 2015 Jun 19;348(6241):1376-81.

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