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I-BET-762

Cat No.
CEI-1363
Description
I-BET-762 is a highly potent inhibitor of bromo and extra C-terminal domain (BET) family with IC50 values of 32.5-42.5 nM.
Product Overview
I-BET-762 is a highly potent inhibitor of BET with IC50 values of 32.5-42.5 nM. I-BET-762 is found to have high affinity with BET (Kd of 50.5-61.3 nM). It binds to the acetyl-lysine (AcK)-binding pocket of BET and competes with AcK. The structure of I-BET-762 allows it to bind with BET in ratio of 2:1 results in the high affinity of it. I-BET-762 also has high selectivity, it has no interaction with other bromodomain-containing proteins. I-BET-762 is reported to downregulate the expression of the genes which are induced by LPS, thus causing the decreased expression of LPS-inducible cytokines and chemokines. In vivo assay shows that I-BET-762 has the anti-inflammatory potential. Treatment of I-BET-762 can cure the mice which have started to develop symptoms of inflammatory disease.
CAS No.
1260907-17-2
Molecular Weight
423.9
Purity
0.9928
Storage
Store at-20°C
Targets
BET
IC50
32.5-42.5 nM
Molecular Formula
C22H22ClN5O2
Chemical Name
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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