UNC1999

UNC1999

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UNC1999 (1431612-23-5) is an orally bioavailable, highly selective inhibitor of both wild-type and mutant EZH1 and EZH2 lysine methyltransferases (IC50‘s = 45 nM and 2 nM respectively).1 Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib (Cat.# 10-1148) in suppressing the proliferation of colon cancer cells

References/Citations:

1) Konze et al. (2013), An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1; ACS Chem. Biol., 8 1324
2) Katona et al. (2014), EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells; Cancer Biol. Ther., 15 1677

CAS:
1431612-23-5

Catalog Number:
10-4542

Activity:
Methyltransferase inhibitor

Chemical 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 Weight:
569.74

Molecular Formula:
C33H43N7O2

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

Physical Properties:
White solid

Purity:
98% by HPLC
NMR (Conforms)

Storage Temperature:
-20°

Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Shipping Code:
RT