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MRK-740 is a potent, selective, substrate-competitive PRDM9 histone methyltransferase inhibitor,IC50 80 nM. MRK-740 is more selective to PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 Reduces PRDM9-Dependent H3K4 Trimethylation (IC50 0.8 μM).
| Molecular Weight | 464.56 |
| Formula | C25H32N6O3 |
| CAS Number | 2387510-80-5 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Abdellah Allali-Hassani, et al. Nat Commun. Discovery of a chemical probe for PRDM9
| Related Histone Methyltransferase Products |
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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. |
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| MS8511
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TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death. |
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