EPZ005687EZH2 inhibitor,potent and selective CAS# 1396772-26-1 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1396772-26-1 | SDF | Download SDF |
| PubChem ID | 60160561 | Appearance | Powder |
| Formula | C32H37N5O3 | M.Wt | 539.67 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 9.4 mg/mL (17.42 mM; Need ultrasonic and warming) | ||
| Chemical Name | 1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide | ||
| SMILES | CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC=C(C=C4)CN5CCOCC5)C6CCCC6)C | ||
| Standard InChIKey | ZOIBZSZLMJDVDQ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C32H37N5O3/c1-21-15-22(2)35-32(39)28(21)18-33-31(38)27-16-25(17-30-29(27)19-34-37(30)26-5-3-4-6-26)24-9-7-23(8-10-24)20-36-11-13-40-14-12-36/h7-10,15-17,19,26H,3-6,11-14,18,20H2,1-2H3,(H,33,38)(H,35,39) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. | |||||
| Targets | EZH2 | |||||
| IC50 | 24 nM (Ki) | |||||
EPZ005687 Dilution Calculator
EPZ005687 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.853 mL | 9.2649 mL | 18.5298 mL | 37.0597 mL | 46.3246 mL |
| 5 mM | 0.3706 mL | 1.853 mL | 3.706 mL | 7.4119 mL | 9.2649 mL |
| 10 mM | 0.1853 mL | 0.9265 mL | 1.853 mL | 3.706 mL | 4.6325 mL |
| 50 mM | 0.0371 mL | 0.1853 mL | 0.3706 mL | 0.7412 mL | 0.9265 mL |
| 100 mM | 0.0185 mL | 0.0926 mL | 0.1853 mL | 0.3706 mL | 0.4632 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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EPZ005687 is a potent inhibitor of EZH2, an enzymatic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of histone H3 lysine 27 (H3K27), that inhibits EZH2 with a value of inhibition constant Ki of 24 nM, which is 500-fold and 50-fold greater in selectivity than 15 other protein methyltransferases and closely related EZH1 respectively. EPZ005687 concentration-dependently inhibits the enzymatic activity of PRC2 with a value of 50% inhibition concentration IC50 of 54 nM through binding to the S-adenosylmethionine (SAM) pocket of the EZH2 SET domain. Study results have shown that EPZ005687 reduces H3K27 methylation in a variety of lymphoma cells and induces apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells.
Reference
Knutson SK, Wigle TJ, Warholic NM, Sneeringer CJ, Allain CJ, Klaus CR, Sacks JD, Raimondi A, Majer CR, Song J, Scott MP, Jin L, Smith JJ, Olhava EJ, Chesworth R, Moyer MP, Richon VM, Copeland RA, Keilhack H, Pollock RM, Kuntz KW. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012 Nov;8(11):890-6.
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[Effects of H3K27 methylation inhibitor EPZ005687 on apoptosis, proliferation and cell cycle of U937 cells and normal CD34 positive cells].[Pubmed:25543475]
Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Dec;22(6):1561-6.
The aim of this study was to investigate the effects of H3K27 methylation inhibitor EPZ005687 on the apoptosis, proliferation and cell cycle of U937 cells and normal CD34(+) cells. The U937 cells and normal CD34(+) cells were treated with different concentration of EPZ005687 at different time points. The apoptosis rate was determined by Annexin V/PI staining. The cell proliferation and cell cycle was determined using WST-1 assay and 7-AAD assay, respectively. The activity of H3K27 methylation was detected by chemiluminescent immunoassay. The results showed that the EPZ005687 induced an obvious apoptosis of U937 cells. The apoptotic rate was 3.96% +/- 0.79%,5.74% +/- 0.73%,13.34% +/- 1.77% and 25.24% +/- 2.55% in U937 cells treated with 0.5, 1, 5 and 10 micromol/L EPZ005687 for 48 hours, respectively. However, EPZ005687 had rare effect on normal bone marrow(NBM) CD34(+) cells. The apoptotic rate was 3.64% +/- 0.62%,4.28% +/- 0.99%,6.18% +/- 1.19% and 7.56% +/- 1.34% after U937 cells were treated with 0.5, 1, 5 and 10 micromol/L EPZ005687 for 48 hours, respectively. EPZ005687 inhibited obviously the proliferation of U937 cells but had weak effect on the proliferation of NBMCD34(+) cells. The inhibitory effect of EPZ005687 on U937 cells was time-dependent after treated with 0.5, 1, 5 and 10 micromol/L EPZ005687 from 12 to 96 hours. EPZ005687 induced G1 phase blocking (G1%, 64.18% +/- 13.27% vs 49.43% +/- 12.54%) and decreased the percentage of cells in S phase (9.67% +/- 2.61% vs15.26% +/- 5.58%) in U937 cells. However, EPZ005687 had no effect on the cell cycle of NBMCD34(+) cells. In addition, EPZ005687 produced obviously depletion of H3K27 methylation in U937 cells (P < 0.05), but hardly had effect on the H3K27 methylation of NBMCD34(+) cells. It is concluded that the EPZ005687 inhibites proliferation, induces apoptosis and cell cycle blocking in G1 phase in leukemia cells. This agent may have potential value in clinical application.
