LKT Labs

Biochemicals for Life Science Research

I-BET151

Product ID I0516
Cas No. 1300031-49-5
Purity ≥98%
Product Unit SizeCostQuantityStock
1 mg $75.30 In stock
5 mg $137.60 In stock
10 mg $202.20 In stock
25 mg $386.30 In stock
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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.

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