dBET57|BRD4 inhibitor|CAS 1883863-52-2|DC Chemicals

Cas No.:	1883863-52-2
Chemical Name:	2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)acetamide
Synonyms:	dBET57,dBET 57,dBET-57
SMILES:	CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)NCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O)C7=CC=C(C=C7)Cl)C
Formula:	C₃₄H₃₁ClN₈O₅S
M.Wt:	699.183
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	dBET57 is a potent and selective heterobifunctional degrader of BRD4 based on the PROTAC technology, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2[1].
Target:	DC50/5h: 500 nM (BRD4BD1)[1]
References:	[1]. Nowak RP, et al. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 2018 Jul;14(7):706-714.

Cat. No.	Product name	Field of application
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DC21360	MZ1	MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers, induces degradation of the BET bromodomain BRD4.
DC21351	MS4078	MS4078 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=11 nM).
DC20367	dTRIM24	dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).
DC21893	dBET57	dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2..
DC12702	A1874	A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).