TNIK&MAP4K4-IN-1 is a dual inhibitor of TNIK and MAP4K4/HGK with IC50s of 1.29 nM and <10 nM, respectively, in human hepaticstellate cell LX-2.
| Molecular Weight | 446.47 |
| Formula | C25H23FN4O3 |
| CAS Number | 2478592-86-6 |
| 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.
[2] Mutsuko Kukimoto-Niino et al. Int J Mol Sci. Structural Insight into TNIK Inhibition
[5] Tesshi Yamada et al. Cancer Sci. Emergence of TNIK inhibitors in cancer therapeutics
| Related MAPKAPK2/MAP3K/MAP4K Products |
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MAP4K4-IN-3 is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, and an IC50 of 470 nM in cell assay. |
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PROTAC MLKL Degrader-1 is a PROTAC degrader of MLKL, with a Dmax ＞90%. |
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HPK1-IN-39 is a selective HPK1 Inhibitor (IC50: 29 nM). |
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