BI 78D3 is a competitive c-Jun N-terminal kinase (JNK) inhibitor (IC50 = 280 nM) that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K. Inhibits JNK interacting protein 1 (JIP1)-JNK binding (IC50 = 500 nM) and prevents JNK substrate phosphorylation. Blocks JNK-dependent Con A-induced liver damage and restores insulin sensitivity in a mouse model of type II diabetes.
| Molecular Weight | 379.37 |
| Formula | C13H9N5O5S2 |
| CAS Number | 883065-90-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 37.94 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.
[1] Steinbach and Akk. J Physiol. Modulation of GABAA receptor channel gating by pentobarbital.
| Related JNK Products |
|---|
| JIP-1(153-163)
JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide). |
| JNK3 inhibitor-5
JNK3 inhibitor-5 is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. |
| JNK-1-IN-1
JNK-1-IN-1 is a JNK-1 inhibitor. |
| JNK2-IN-1
JNK2-IN-1 is a JNK2 inhibitor (Kds: 79.2 μM). |
| JNK-1-IN-2
JNK-1-IN-2 is a JNK-1 inhibitor (IC50: 33.5 nM). |
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