Name: I-BET-762
Price: 252.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    I-BET-762 is a highly potent inhibitor of BET with IC50 values of 32.5–42.5 nM [1].
    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 [1].
    
    [1] Nicodeme E, Jeffrey KL, Schaefer U, Beinke S, Dewell S, Chung CW, Chandwani R, Marazzi I, Wilson P, Coste H, White J, Kirilovsky J, Rice CM, Lora JM, Prinjha RK, Lee K, Tarakhovsky A. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468 (7327):1119-23.
- Properties
  - Alternative 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
    
    CAS Number
    
    1260907-17-2
    
    Molecular Formula
    
    C22H22ClN5O2
    
    Molecular Weight
    
    423.9
    
    Appearance
    
    A solid
    
    Purity
    
    99.28%
    
    Solubility
    
    ≥21.19 mg/mL in DMSO; insoluble in H2O; ≥13.93 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Xu Y, Wu Y, et al. "A Tumor-Specific Super-Enhancer Drives Immune Evasion by Guiding Synchronous Expression of PD-L1 and PD-L2." Cell Rep. 2019 Dec 10;29(11):3435-3447.e4. PMID:31825827
    2. Peter J. Thompson, Ajit Shah, et al. "BET proteins are required for transcriptional activation of the senescent beta cell secretome in Type 1 Diabetes." bioRxiv. 2019 August 15.
    3. Kim SR, Lewis JM, et al. "BET inhibition in advanced cutaneous T cell lymphoma is synergistically potentiated by BCL2 inhibition or HDAC inhibition." Oncotarget. 2018 Jun 26;9(49):29193-29207. PMID:30018745
    4. Yang R, Wu Y, et al. "A super-enhancer maintains homeostatic expression of Regnase-1." Gene. 2018 May 16. pii: S0378-1119(18)30542-0. PMID:29777912
    5. Fontanals-Cirera B, Hasson D, et al. "Harnessing BET Inhibitor Sensitivity Reveals AMIGO2 as a Melanoma Survival Gene." Mol Cell. 2017 Nov 16;68(4):731-744.e9. PMID:29149598
    6. Ronald M. Evans,Michael Downes,et al. "Increasing storage of vitamin a, vitamin d and/or lipids." US Patent App. 15, 2016.

I-BET-762

I-BET-762

Background

We Also Recommend

Estradiol Cypionate

I-BET151 (GSK1210151A)

RVX-208