I-BET762 (GSK525762), BET Inhibitor


Catalog No. size PriceQuantity
M60154-2D 10 mM in DMSO (0.472 mL) $139
M60154-2S 2mg solid $139
M60154-10S 10 mg solid $570

Description

Product Information
Molecular Weight: 423.90
Formula: C22H22ClN5O2
Purity: ≥98%
CAS#: 1260907-17-2
Solubility: DMSO up to 50 mM
Chemical Name: (S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

I-BET762 (GSK525762) is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~35 nM. It suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation. It is highly selective over other bromodomain-containing proteins. In vivo studies using I-BET762 have demonstrated efficacy in a range of oncology and immunoinflammatory models. I-BET762 is currently in clinical development for oncology indication. 

 

How to Use: 

 

  • In vitro:  I-BET762 was used at 0.5-1 µM final concentration in various in vitro assays.
  • In vivo: I-BET762 could be dosed to the mice by oral administration at 10-30 mg/kg once per day. 

 

 

Reference:

  • 1. Mirguet O, et al. Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. (2013) J Med Chem. 56(19):7501-15.
  • 2. Zhao Y, et al. The making of I-BET762, a BET bromodomain inhibitor now in clinical development. (2013) J Med Chem. 56(19):7498-500. 

 

Products are for research use only. Not for human use.

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