BRD4770

BRD4770 is a novel histone methyltransferase inhibitor. BRD4770 reduced cellular levels of di- and trimethylated H3K9 without inducing apoptosis, induced senescence, and inhibited both anchorage-dependent and -independent proliferation in the pancreatic cancer cell line PANC-1. ATM-pathway activation, caused by either genetic or small-molecule inhibition of G9a, may mediate BRD4770-induced cell senescence. BRD4770 may be a useful tool to study G9a and its role in senescence and cancer cell biology.

Product information

CAS Number: 1374601-40-7

Molecular Weight: 413.47

Formula: C25H23N3O3

Synonym:

BRD-4770

BRD4770

BRD 4770

Chemical Name: methyl 2-benzamido-1-(3-phenylpropyl)-1H-benzo[d]imidazole-5-carboxylate

Smiles: COC(=O)C1C=C2N=C(NC(=O)C3C=CC=CC=3)N(CCCC3C=CC=CC=3)C2=CC=1

InChiKey: UCGWYCMPZXDHNR-UHFFFAOYSA-N

InChi: InChI=1S/C25H23N3O3/c1-31-24(30)20-14-15-22-21(17-20)26-25(27-23(29)19-12-6-3-7-13-19)28(22)16-8-11-18-9-4-2-5-10-18/h2-7,9-10,12-15,17H,8,11,16H2,1H3,(H,26,27,29)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

BRD4770 (0-20 µM; 72 hours; PANC-1 cells) treatment reduces the number of cells after 72 h. BRD4770 (2.5-5 µM; 24 hours; PANC-1 cells) treatment decreases H3K9 trimethylation level by 23% in PANC-1 cells. BRD4770 induces a senescent phenotype in a pancreatic cancer cell line. BRD4770 also inhibits both anchorage-dependent and -independent cell proliferation and induces G2/M cell-cycle arrest. BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway without inducing DNA damage, while the ataxia telangiectasia and Rad3-related protein (ATR) pathway is not affected. BRD4770 also induces increased levels of lysine acetylation in cells without inhibiting histone deacetylases.

References:

1. Yuan Y, Tang AJ, Castoreno AB, Kuo SY, Wang Q, Kuballa P, Xavier R, Shamji AF, Schreiber SL, Wagner BK. Gossypol and an HMT G9a inhibitor act in synergy to induce cell death in pancreatic cancer cells. Cell Death Dis. 2013 Jun 27;4:e690. doi: 10.1038/cddis.2013.191. PubMed PMID: 23807219; PubMed Central PMCID: PMC3702302.

Products are for research use only. Not for human use.