A synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM); disrupts binding of BET proteins with acetylated histones

I-BET762 – 10 mg

Brand:
Cayman
CAS:
1260907-17-2
Storage:
-20
UN-No:
Non-Hazardous - /

The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, affect inflammatory gene expression by controlling the assembly of histone acetylation-dependent chromatin complexes.{19558,19559} I-BET762 is a synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM).{18802,28490} It blocks binding of BET proteins with acetylated histones, disrupting the formation of chromatin complexes involved in the expression of specific inflammatory genes in activated macrophages.{18802} Through these actions, I-BET762 provides protection against bacteria-induced sepsis and lipopolysaccharide-triggered endotoxic shock.{18802}  

 

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SKU: 10676 - 10 mg Category:

Description

A synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM); disrupts binding of BET proteins with acetylated histones, suppressing the expression of specific inflammatory genes involved in sepsis and endotoxic shock

Formal name: (S)-2-(6-(4-chlorophenyl)-8-methoxy-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide

Synonyms:  GSK525762A

Molecular weight: 423.9

CAS: 1260907-17-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains||Research Area|Immunology & Inflammation|Innate Immunity|Pattern Recognition||Research Area|Immunology & Inflammation|Innate Immunity|Sepsis/Shock

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