UNC1999, Methyltransferase inhibitor (TBI4542)

Description

Product Details

Formal Name: N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide

Molecular Formula: C₃₃H₄₃N₇O₂

Formula Weight: 569.74

CAS Number: 1431612-23-5

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 10 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

Methyltransferase inhibitor

Functions

UNC1999 is an orally active, highly selective inhibitor of both wild-type and mutant EZH1 and EZH2 lysine methyltransferases (IC50’s = 45 nM and 2 nM respectively). Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib in suppressing the proliferation of colon cancer cells. It suppresses global H3K27 trimethylation/demethylation and inhibits the growth of mixed lineage leukemia (MLL)-rearranged leukemia cells.

Application Procedures

First dissolved in DMSO (up to 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 3 months.