All AbMole products are for research use only, cannot be used for human consumption.
Tazemetostat (EPZ-6438) hydrobromide is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
In vivo, Tazemetostat (250 or 500 mg/kg; twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors.
| Molecular Weight | 653.65 |
| Formula | C34H45BrN4O4 |
| CAS Number | 1467052-75-0 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone Methyltransferase Products |
|---|
| WDR5-IN-4
WDR5-IN-4 is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity. |
| CMP-5 dihydrochloride
CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. |
| MS67
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. |
| MS8511
MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). |
| TM2-115
TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
