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MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intracellular H3K9me2 levels.MS8511 can be used to study a wide range of cancers including brain, breast, and ovarian cancers .
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $195 | In Stock | |
5 mg | $483 | In Stock | |
10 mg | $692 | In Stock | |
25 mg | $1,080 | In Stock | |
50 mg | $1,490 | In Stock | |
100 mg | $1,970 | In Stock |
Description | MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intracellular H3K9me2 levels.MS8511 can be used to study a wide range of cancers including brain, breast, and ovarian cancers . |
Targets&IC50 | G9a:44 nM (Kd), G9a:100 nM, GLP:46 nM (Kd), GLP:140 nM |
In vitro | MS8511 HCl (Compound 8), within a range of 0-100 μM over 10 minutes, selectively inhibits G9a and GLP compared to other PKMTs and PRMTs, with IC50 values of 100 nM (G9a) and 140 nM (GLP) [1].With a duration of 50 minutes, MS8511 HCl exhibits a preference for covalent modification of G9a over GLP, with Kd values of 44 nM (G9a) and 46 nM (GLP) [1].Over a range of 0-5 μM and durations of 24-72 hours,MS8511 HCl effectively reduces the H3K9me2 mark in MDA-MB-231 and K562 cells [1]. At concentrations ranging from 0.8 to 25 μM over a period of 3 days, MS8511 HCl inhibits the growth of MDA-MB-231 cells [1]. |
Alias | MS8511 HCl(2866408-21-9 Free base) |
Molecular Weight | 532.12 |
Formula | C28H42ClN5O3 |
Smiles | O=C(NC1=CC(NC2CCN(C(C)C)CC2)=C3C=C(OC)C(OCCCN4CCCC4)=CC3=N1)C=C.Cl |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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