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A-196 is a potent selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively, and biochemically inhibits SUV4-20 in a substrate-competitive manner. In addition, A-196 is a first-in-class chemical probe for SUV4-20, which can be used to study the role of histone methyltransferases in genome integrity.
| Molecular Weight | 359.25 |
| Formula | C18H16Cl2N4 |
| CAS Number | 1982372-88-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 7.18 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Xiao-Ying Zhang, et al. Scorpion venoms in gastric cancer
[4] Yang Cao, et al. miR-196 acts as a tumor suppressor in osteosarcoma by targeting HOXA9
| 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. |
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