UNC1999 , ≥98% , 1431612-23-5

Synonym(s):
1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide

CAS NO.：1431612-23-5

Empirical Formula: C33H43N7O2

Molecular Weight: 569.74

MDL number: MFCD26960958

PRODUCT Properties

• Boiling point: 804.7±65.0 °C(Predicted)
• Density: 1.23±0.1 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: DMSO: soluble15mg/mL, clear
• pka: 11.84±0.10(Predicted)
• form: powder
• color: white to beige
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
• InChIKey: DPJNKUOXBZSZAI-UHFFFAOYSA-N
• CAS DataBase Reference: 1431612-23-5

Description and Uses

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

The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. UNC1999 is a cell-permeable EZH2 inhibitor (IC50 = 2 nM) that is 22-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases. UNC1999 has been shown to inhibit H3K27 methylation in MCF10A cells with an IC50 value of 124 nM.[Cayman Chemical]

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338
• Hazard Codes: Xn
• Risk Statements: 22
• WGK Germany: 3