WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407812
Description: ZBC260, also known as BETd-260, is a potent and selective BET inhibitor or BET degrader. ZBC260 effectively degrades BRD4 protein at concentrations as low as 30 pM in the RS4;11 leukemia cell line, achieves an IC50 value of 51 pM in inhibition of RS4;11 cell growth and induces rapid tumor regression in vivo against RS4;11 xenograft tumors. ZBC260 is a highly potent and efficacious BET degrader.
MedKoo Cat#: 407812
Chemical Formula: C43H46N10O6
Exact Mass: 798.3602
Molecular Weight: 798.905
Elemental Analysis: C, 64.65; H, 5.80; N, 17.53; O, 12.02
Synonym: ZBC260; ZBC 260; ZBC-260; BETd-260; BETd 260; BETd260.
IUPAC/Chemical Name: 4-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pentyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
InChi Key: UZXANFBIRSYHGO-UHFFFAOYSA-N
InChi Code: InChI=1S/C43H46N10O6/c1-5-53-34(20-30(50-53)25-13-14-25)46-39-37-27-19-33(58-4)28(36-22(2)51-59-23(36)3)18-31(27)45-38(37)48-40(49-39)42(56)44-17-8-6-7-10-24-11-9-12-26-29(24)21-52(43(26)57)32-15-16-35(54)47-41(32)55/h9,11-12,18-20,25,32H,5-8,10,13-17,21H2,1-4H3,(H,44,56)(H,47,54,55)(H2,45,46,48,49)
SMILES Code: O=C(N1)CCC(N(CC2=C3C=CC=C2CCCCCNC(C4=NC5=C(C(NC6=CC(C7CC7)=NN6CC)=N4)C8=CC(OC)=C(C9=C(C)ON=C9C)C=C8N5)=O)C3=O)C1=O
The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic "readers" and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases. Recently, heterobifunctional small-molecule BET degraders have been designed based upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation
1: Zhou B, Hu J, Xu F, Chen Z, Bai L, Fernandez-Salas E, Lin M, Liu L, Yang CY,
Zhao Y, McEachern D, Przybranowski S, Wen B, Sun D, Wang S. Discovery of a
Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with
Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med
Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816. [Epub ahead of print]
PubMed PMID: 28339196.