Chemical Property of UNC 1999
Chemical Property:
- Boiling Point:804.7±65.0 °C(Predicted)
- PKA:11.84±0.10(Predicted)
- PSA：99.41000
- Density:1.23±0.1 g/cm3(Predicted)
- LogP:5.89490
- Storage Temp.:2-8°C
- Solubility.:DMSO: soluble15mg/mL, clear
- Purity/Quality:
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99%, *data from raw suppliers
UNC1999 *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xn
- Hazard Codes:Xn
- Statements:
22
- MSDS Files:
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SDS file from LookChem
Useful:
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Description
UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. 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
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Uses
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] UNC1999 acts as an inhibitor for lysine methyltransferases EZH2 and EZH1 which have been implicated in the expression of various cancers.
