I-BET151

Product ID I0516

Cas No. 1300031-49-5

Purity ≥98%

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Product Info
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Description
Product Info
Shipping and Storage
Downloads
References
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Description

I-BET-151 is a BET bromodomain (BRD) inhibitor that inhibits BRD2, BRD3, and BRD4. I-BET-151 exhibits anticancer chemotherapeutic and anti-inflammatory activities. In vitro and in vivo, this compound induces apoptosis and inhibits cellular proliferation in various cancer models. I-BET-151 inhibits recruitment of the P-TEFb component of cyclin-dependent kinase 9 (CDK9) to chromatin, causing transcriptional regression of Myc. I-BET-151 also inhibits bacteria-induced inflammation and sepsis in animal models.

Product Info

Cas No.	1300031-49-5
Purity	≥98%
Formula	C₂₃H₂₁N₅O₃
Formula Wt.	415.44
IUPAC Name	7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-pyridin-2-ylethyl]-3H-imidazo[4,5-c]quinolin-2-one
Synonym	GSK-1210151A, GSK1210151A
Solubility	Ethanol 27 mg/mL (64.99 mM) DMSO Insoluble Water Insoluble
Appearance	White to off white powder

Shipping and Storage

Store Temp	-20°C
Ship Temp	Ambient

Downloads

MSDS	I0516 MSDS PDF
Info Sheet	I0516 Info Sheet PDF

References

Chaidos A, Caputo V, Gouvedenou K, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705. PMID: 24335499.

Seal J, Lamotte Y, Donche F, et al. Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. PMID: 22437115.