UNC1999

Aliases: 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
Catalog No: 14114 Format: 25 mg $240 Buy
Catalog No: 14115 Format: 5 mg $60 Buy
Application: Histone Methylation (HMT & HDM)

Chemical Properties

MW = 569.7
C33H43N7O2
CAS 1431612-23-5
>98% (HPLC); NMR (Conforms)

Description

UNC1999 is an orally active, highly selective inhibitor of both wild-type and mutant EZH1 and EZH2 lysine methyltransferases (IC50 = 45 nM and 2 nM respectively)(ref 1). Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib in suppressing the proliferation of colon cancer cells (ref 2). It suppresses global H3K27 trimethylation/demethylation and inhibits the growth of mixed lineage leukemia (MLL)-rearranged leukemia cells (ref 3).

Contents

White powder. May be dissolved in DMSO (10 mg/ml).

Storage Conditions

Store desiccated as supplied at -20° for up to 2 years. Store solutions at -20°C for up to 3 months.

References

1. KD Konze et al. ACS Chem. Biol. 2013, 8:1324
2. BW Katona et al. Cancer Biol. Ther. 2014, 15:1677
3. B Xu et al. Blood 2015, 125:346

 
Chemical structure of UNC1999.

Chemical structure of UNC1999.