N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide UNC1999
UNC1999
CAS: 1431612-23-5
Molecular Formula: C33H43N7O2
N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide UNC1999 - Names and Identifiers
N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide UNC1999 - Physico-chemical Properties
| Molecular Formula | C33H43N7O2 |
| Molar Mass | 569.74 |
| Density | 1.23±0.1 g/cm3(Predicted) |
| Boling Point | 804.7±65.0 °C(Predicted) |
| Solubility | DMSO: soluble15mg/mL, clear |
| Appearance | powder |
| Color | white to beige |
| pKa | 11.84±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| In vitro study | UNC1999 had strong inhibitory activity against EZH2 Y641 and EZH2 Y641F mutants in vitro. UNC1999 concentration-dependently reduced the level of H3K27me3 in the MCF10A cell line with an IC50 of 124 nM, resulting in lower cytotoxicity. UNC1999 showed effective concentration-dependent inhibition of cell proliferation in the DLBCL cell line containing the EZH2Y641N mutation. In addition, biotinylated UNC1999 allows EZH2 to be isolated from HEK293T cell lysates and can therefore be used in chemoproteomics studies. UNC1999 has strong inhibitory activity against EZH2 Y641 and EZH2 Y641F mutants in vitro. UNC1999 concentration-dependently reduced the level of H3K27me3 in the MCF10A cell line with an IC50 of 124 nM, resulting in lower cytotoxicity. UNC1999 showed effective concentration-dependent inhibition of cell proliferation in the DLBCL cell line containing the EZH2Y641N mutation. In addition, biotinylated UNC1999 allows EZH2 to be isolated from HEK293T cell lysates and can therefore be used in chemoproteomics studies. |
| In vivo study | In vivo treatment with UNC1999 (150 and 50 mg/kg, I. p.) maintained plasma concentrations above their cellular IC50 values for more than 24 hours. In addition, UNC1999 has Oral activity on mice, which can be used for chronic animal experiments more practical and convenient. In vivo treatment with UNC1999 (150 and 50 mg/kg, I. p.) maintained plasma concentrations above their cellular IC50 values for more than 24 hours. In addition, UNC1999 has Oral activity on mice, which can be used for chronic animal experiments more practical and convenient. |
N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide UNC1999 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| WGK Germany | 3 |
N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide UNC1999 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.755 ml | 8.776 ml | 17.552 ml |
| 5 mM | 0.351 ml | 1.755 ml | 3.51 ml |
| 10 mM | 0.176 ml | 0.878 ml | 1.755 ml |
| 5 mM | 0.035 ml | 0.176 ml | 0.351 ml |
Last Update：2024-01-02 23:10:35
N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide UNC1999 - Reference Information
| biological activity | UNC1999 an effective EZH1 and EZH2 selective inhibitor with oral activity, its IC50 is 2 nM and 45 nM respectively, and its selectivity for many epigenetically related or unrelated targets is greater than 1000 times. UNC1999 is an effective selective inhibitor of EZH2 and EZH1 with oral activity. IC50 in cell-free test is 2 nM and 45 nM respectively, and the selectivity for extensive epigenetically related or unrelated targets is greater than 1000 times. UNC1999 is an effective inducer of autophagy autophagy. UNC1999 can specifically inhibit H3K27me3/2 and induce a series of anti-leukemia effects, including anti-proliferation, differentiation and apoptosis. |
| in vitro study | UNC1999 has strong inhibitory activity against EZH2 Y641 and EZH2 Y641F mutants in vitro. UNC1999 concentration-dependent reduction of the level of H3K27me3 in the MCF10A cell line, its IC50 was 124 nM, resulting in lower cytotoxicity. UNC1999 showed effective concentration-dependent inhibition of cell proliferation in DLBCL cell lines containing EZH2Y641N mutations. In addition, biotinylated UNC1999 can separate EZH2 from HEK293T cell lysate, so it can be used in chemical proteomics research. UNC1999 has strong inhibitory activity on EZH2 Y641 and EZH2 Y641F mutants in vitro. UNC1999 concentration-dependent reduction of the level of H3K27me3 in the MCF10A cell line, its IC50 was 124 nM, resulting in lower cytotoxicity. UNC1999 showed effective concentration-dependent inhibition of cell proliferation in DLBCL cell lines containing EZH2Y641N mutations. In addition, biotinylated UNC1999 can separate EZH2 from HEK293T cell lysate, so it can be used in chemical proteomics research. |
| in vivo study | UNC1999 (150 and 50 mg/kg, I. p.) in vivo treatment kept it in plasma for more than 24 hours at a concentration higher than its cell IC50 value. In addition, UNC1999 have oral activity on mice, which can be more practical and convenient for chronic animal experiments. UNC1999 (150 and 50 mg/kg, I. p.) is treated in vivo to keep it in plasma for more than 24 hours at a concentration higher than its cell IC50 value. In addition, UNC1999 have oral activity on mice, which can be more practical and convenient for chronic animal experiments. |
| features | the first oral active EZH1, EZH2 inhibitor |
| target | TargetValue EZH2 (Cell-free say) 2 nM EZH1 (Cell-free say) 45 nM |
| Target | Value |
| EZH2 (Cell-free assay) | 2 nM |
| EZH1 (Cell-free assay) | 45 nM |
Last Update：2024-04-09 20:49:11
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Spot supply
Product Name: UNC1999 Visit Supplier Webpage Request for quotationCAS: 1431612-23-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide UNC1999
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