TC ASK 10 is a potent ASK1 inhibitor (IC50 = 14 nM); displays selectivity for ASK1 over other kinases including ASK2 (IC50 = 0.51 μM), MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf (IC50 values are > 10 μM). Blocks downstream JNK1/p38 phosphorylation in cells. Orally bioavailable.
| Molecular Weight | 432.35 |
| Formula | C21H21N5O.2HCl |
| CAS Number | 1005775-56-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 43.23 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] Freissmuth, et al. Mol Pharmacol. Suramin analogues as subtype-selective G protein inhibitors.
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| BSJ-04-122
BSJ-04-122 is a covalent MKK4/7 dual inhibitor. BSJ-04-122 inhibits MKK4 and MKK7 with IC50 values of 4 nM and 181 nM, respectively. |
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