Product Name

OTX015

General description

OTX015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays.

Synonym

Birabresib; MK-8628

Purity

≥98.5%(HPLC)

CAS Number

202590-98-5

Formula

C²⁵H²²ClN⁵O²S

Molecular Weight

491.99

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White to Light brown Solid

Solubility(25°C)

DMSO

≥50mg/ml

Ethanol

≥50mg/ml

Water

Very slightly soluble

l  Biological Information

Biochem/Physiol  Actions

Birabresib is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity. Upon administration, birabresib binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene . Prevention of the of certain growth-promoting genes, including c-Myc-dependent target genes, may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, the BET proteins BRD2, BRD3, BRD4 are transcriptional regulators that play an important role in cellular growth.

l  Storage

Storage temp.

-20°C

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov