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UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.
Nucleic Acids Res. 2022 Aug 12;50(14):7938-7958.
HDAC1 and PRC2 mediate combinatorial control in SPI1/PU.1-dependent gene repression in murine erythroleukaemia
UNC1999 purchased from AbMole
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Source | Cell Death Dis (2018). Figure 2. UNC1999 |
| Method | western blot | |
| Cell Lines | VSMCs | |
| Concentrations | 5 μM | |
| Incubation Time | 24 h | |
| Results | Important to note that UNC1999 stimuli resulted in VSMC numbers visibly reducing as early as 24 h |
| Cell Experiment | |
|---|---|
| Cell lines | DLBCL cell line harboring the EZH2Y641N mutant |
| Preparation method | DB cells, a diffuse-large B-cell lymphoma cell line harboring the EZH2 Y641N mutation, are obtained from ATCC and cultured in RPMI 1640 supplemented with 10% fetal bovine serum, antibiotics, and various concentrations of compounds (DMSO control, UNC1999, or UNC2400). The medium which contains the test compound or control is refreshed every 3 days. Using TC20 automated cell counter system to measure the numbers of viable cells from at least three independent experiments . Total histones are prepared from cell nuclei using an acidic extraction protocol. About 1 μg of total histones is separated using 15% SDS-PAGE, transferred to PVDF membranes, and probed with histone antibodies. Antibodies used in this study are those against EZH2, general H3, and H3K27me3 |
| Concentrations | ~5 μM |
| Incubation time | 8 days |
| Animal Experiment | |
|---|---|
| Animal models | Male Swiss albino mice |
| Formulation | DMSO |
| Dosages | ~150 mg/kg (i.p.), ~50 mg/kg (oral) |
| Administration | Intraperitoneal administration or oral administration |
| Molecular Weight | 569.74 |
| Formula | C33H43N7O2 |
| CAS Number | 1431612-23-5 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Naoya Mimura. Novel epigenetic therapies for multiple myeloma
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| EPZ005687
EPZ005687 is a potent, selective EZH2 inhibitor,Ki The value is 24 nM, which is 50 times more selective than EZH1 and 500 times more selective than 15 other methyltransferases. |
| GSK343
GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. |
| CPI-169 racemate
CPI-169 racemate is the racemate form of CPI-169, which is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2); decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines. |
| MS1943
MS1943 is a pioneering oral bioactive selective EZH2 inhibitor with an IC50 of 120 nM. MS1943 significantly reduced EZH2 protein levels in many triple negative breast and other cancers and non-cancer lines. MS1943 effectively blocked the proliferation of multiple triple negative breast cancers and other cancer lines. |
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