Nexinhib20 is an inhibitor of the protein-protein interaction between the small GTPase Rab27a and its effector JFC1 (IC50 = 2.6 µM). Nexinhib20 inhibits myeloperoxidase (MPO) secretion induced by granulocyte macrophage colony-stimulating factor (GM-CSF) and fMLP in isolated human neutrophils (IC50 = 0.33 µM).
Nexinhib20 (30 mg/kg) reduces LPS-induced increases in plasma MPO levels, as well as LPS-induced hepatic and renal neutrophil infiltration in a mouse model of endotoxin-induced systemic inflammation.
| Molecular Weight | 300.3 |
| Formula | C15H16N4O3 |
| CAS Number | 331949-35-0 |
| Solubility (25°C) | DMSO 30 mg/mL Ethanol 15 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 GTPase Products |
|---|
| NSC23766 trihydrochloride
NSC23766 3HCl is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM; does not inhibit the closely related targets, Cdc42 or RhoA. |
| EHop-016
EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1, equally potent inhibition for Rac3. |
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