dbet6

InvivoChem Cat #:V3477CAS #:1950634-92-0Purity >=98%

Description: dBET6 is a novel, highly potent, selective and cell-permeable chemical degrader of BET bromodomain proteins based on PROTAC technology with an IC50 of 14 nM. It has potential antitumor activity. In contrast to the selective effect of bromodomain inhibition on transcription, BET degradation prompts a collapse of global elongation that phenocopies CDK9 inhibition. Notably, BRD4 loss does not directly affect CDK9 localization. These studies, performed in translational models of T cell leukemia, establish a mechanism-based rationale for the development of BET bromodomain degradation as cancer therapy.

References: Mol Cell. 2017 Jul 6; 67(1):5-18.e19

-20C for 3 years in powder form

Synonym: dBET6; d BET6; d-BET6
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-(8-(2-((2-(2, 6-dioxopiperidin-3-yl)-1, 3-dioxoisoindolin-4-yl)oxy)acetamido)octyl)-acetamide
InChi Key: JGQPZPLJOBHHBK-UFXYQILXSA-N
InChi Code: InChI=1S/C42H45ClN8O7S/c1-23-24(2)59-42-35(23)37(26-13-15-27(43)16-14-26)46-29(38-49-48-25(3)50(38)42)21-33(53)44-19-8-6-4-5-7-9-20-45-34(54)22-58-31-12-10-11-28-36(31)41(57)51(40(28)56)30-17-18-32(52)47-39(30)55/h10-16, 29-30H, 4-9, 17-22H2, 1-3H3, (H, 44, 53)(H, 45, 54)(H, 47, 52, 55)/t29-, 30?/m0/s1
SMILES Code: O=C(NCCCCCCCCNC(COC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[CH]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N41