NAE-IN-M22 is a potent, selective, and reversible inhibitor of NEDD8-activating enzyme (NAE) in the micromolar range. In addition, NAE-IN-M22 inhibits the growth of various cancer cells and induces apoptosis in A549 cells.
| Molecular Weight | 363.32 |
| Formula | C20H24Cl2N2 |
| CAS Number | 864420-54-2 |
| Form | Solid |
| Solubility (25°C) | DMSO >100 mg/mL |
| 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.
| Related NEDD8-activating Enzyme Products |
|---|
| ZM223 hydrochloride
ZM223 hydrochloride is a potent, orally active, non-covalent NEDD8 activating enzyme (NAE) inhibitor. |
| TAS4464 hydrochloride
TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM. |
| Pevonedistat hydrochloride
Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM. |
| TAS4464
TAS4464 is a highly selective inhibitor of NEDD8 activated enzyme (NAE),IC50 The value is 0.955 nM. |
| Pevonedistat (MLN4924)
Pevonedistat (MLN4924) is a first-of-its-kind (first-in-class) small molecule inhibitor of Nedd8 activating enzyme (NAE) with an IC50 of 4 nM. |
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