NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor. NIH-12848 inhibited PI5P4Kγ with an IC50 of approximately 1 μM but did not inhibit the α and β PI5P4K isoforms at concentrations up to 100 μM. NIH-12848 inhibits the translocation of Na+/ K+-ATPase to the plasma membrane that occurs when mpkCCD cells grow to confluence and also prevents reversibly their forming of ‘domes’ on the culture dish. NIH-12848 is a potentially powerful tool for exploring the cell physiology of PI5P4Ks.
| Molecular Weight | 385.41 |
| Formula | C20H14F3N3S |
| CAS Number | 959551-10-1 |
| Solubility (25°C) | DMSO: ≥ 25 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 PI5P4K Products |
|---|
| CC260
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Ki values of 40 nM and 30 nM, respectively, and can be used in cellular energy metabolism, diabetes, and cancer research. |
| THZ-P1-2
THZ-P1-2 is a first-in-class, selective PI5P4K inhibitor with an IC50 of 190 nM for Pi5P4α. |
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