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I-BET-762 BET inhibitor,highly potent

Catalog No.B1498
Size Price Stock Qty
10mM (in 1mL DMSO)
$95.00
In stock
5mg
$88.00
In stock
10mg
$135.00
In stock
50mg
$450.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. 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
2. 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
3. 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
4. Ronald M. Evans,Michael Downes,et al. "Increasing storage of vitamin a, vitamin d and/or lipids." US Patent App. 15, 2016.

Quality Control

Chemical structure

I-BET-762

Related Biological Data

I-BET-762

Related Biological Data

I-BET-762

Related Biological Data

I-BET-762

Biological Activity

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.
Targets BET          
IC50 32.5–42.5 nM          

Protocol

Kinase experiment [1]:

Fluorescence resonance energy transfer (FRET) titrations

I-BET is titrated against BRD2 (200 nM), BRD3 (100 nM) and BRD4 (50 nM) in 50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS in the presence of tetra-acetylated Histone H4 peptide (200 nM). After equilibrating for 1 hour, the bromodomain protein : peptide interaction is detected using FRET following the addition of 2nM Europium cryptate labelled streptavidin and 10 nM XL-665-labelled anti-6His antibody in assay buffer c

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Chemical Properties

Cas No. 1260907-17-2 SDF Download SDF
Synonyms N/A
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
Canonical SMILES CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C
Formula C22H22ClN5O2 M.Wt 423.9
Solubility >21.2mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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].

References:
[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.