All AbMole products are for research use only, cannot be used for human consumption.
AZ505 ditrifluoroacetate is a potent and highly selective inhibitor of the oncogenic protein SMYD2 (IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM); EZH2(IC50>83.3 uM). The inhibition constant for AZ505 was determined to be 0.30 mM using Michaelis-Menten kinetics. A single AZ505 molecule is bound in the peptide binding groove of SMYD2. The cyclohexyl group of AZ505 is positioned in a primaryhydrophobic pocket that is formed at the interface of the core SET and I-SET domains, which is occupied by residue L369 of the p53 peptide. AZ505 has an IC50 value of 0.12 uM against SMYD2, and has no potency against SMYD3.
| Molecular Weight | 805.59 |
| Formula | C33H40Cl2F6N4O8 |
| CAS Number | 1035227-44-1 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 85 mg/mL |
| Storage | 4°C, dry, sealed |
| Related Histone Methyltransferase Products |
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| 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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