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 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. |
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| C21
C21 is a potent, irreversible, and selective PRMT1 inhibitor with an IC50 of 1.8 μM. |
| EZH2-IN-15
EZH2-IN-15 (SHR2554) is a EZH2 inhibitor. |
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