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Chemical Structure : MRK-740
CAS No.: 2387510-80-5
Catalog No.: PC-73122Not For Human Use, Lab Use Only.
MRK-740 (MRK740) is a first-in-class, potent, selective and cell-active PRDM9 inhibitor with IC50 of 80 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $138 | In stock | |
| 10 mg | $218 | In stock | |
| 25 mg | $398 | In stock | |
| 50 mg | $588 | In stock | |
| 100 mg | Get quote |
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MRK-740 (MRK740) is a first-in-class, potent, selective and cell-active PRDM9 inhibitor with IC50 of 80 nM.
MRK-740 is much less potent at inhibiting PRDM7 (IC50=45 uM), doest not inhibits 11 other PRDM family members, also shows selectivity against a panel of 108 enzymes and receptors.
MRK-740 binds in the substrate-binding pocket (SPR Kd=87 nM), with unusually extensive interactions with the cofactor SAM, conferring SAM-dependent substrate-competitive inhibition.
MRK-740 engages PRMD9 and inhibits PRDM9-dependent trimethylation of ectopic H3K4 (EC50=0.8 uM) and endogenous H3K4 in in HEK293T cells, with minimal impact on cell viability.
MRK-740 specifically inhibits PRDM9-dependent methylation on endogenous chromatin, but does not affect H3K4 methylation activity from non-PRDM9 sources.
MRK-740 does not affect proliferation of cancer cell lines.
MRK-740 is a chemical probe for the PRDM subfamily of methyltransferases.
| M.Wt | 464.57 | |
| Formula | C25H32N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-(3,5-Dimethoxyphenyl)-5-(1-methyl-9-(2-methylpyridin-4-yl)-1,4,9-triazaspiro[5.5]undecan-4-yl)-1,2,4-oxadiazole |
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1. Allali-Hassani A, et al. Nat Commun. 2019 Dec 17;10(1):5759.
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