AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50 values of 150, 220, and 70 nM for JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 and Clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo-2 colon cancer cells.
In vivo, AS601245 (40, 60, and 80 mg/kg; i.p.) provides significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia. AS601245 (0.3-10 mg/kg; p.o.) is a potent inhibitor of LPS-induced TNF-α release in mice.
| Molecular Weight | 372.45 |
| Formula | C20H16N6S |
| CAS Number | 345987-15-7 |
| Solubility (25°C) | DMSO 6 mg/mL (May need ultrasonic) |
| 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 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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