PF 5006739 is a potent, selective CK1δ/ε inhibitor with IC50s of 3.9 nM and 17.0 nM, respectively, and possesses low nanomolar CK1δ/ε potency in vitro and high kinome selectivity. In addition, PF-5006739 improves glucose tolerance in diet-induced obesity (DIO) and genetic (ob/ob) mouse models. It can be used in studies of psychiatric disorders.
| Molecular Weight | 419.46 |
| Formula | C22H22FN7O |
| CAS Number | 1293395-67-1 |
| Solubility (25°C) | DMSO 41.95 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.
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ON 108600 is an inhibitor of CK2 (Casein Kinase2)/TNIK/DYRK1 with IC50 values of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM for DYRK1A/DYRKB, DYRK2, CK2α1/CK2α2, and TNIK, respectively. 0.005 μM. It has anti-tumor activity. |
| (R)-DRF053 dihydrochloride
(R)-DRF053 dihydrochloride is a potent inhibitor of casein kinase 1 (CK1), CDK1/cyclin B, and CDK5/p25, with IC50s of 14 nM, 220 nM, and 80 nM, respectively.(R)-DRF053 dihydrochloride prevented the production of CK1-dependent amyloid-β in cellular models. In addition, (R)-DRF053 dihydrochloride prevented the production of CK1-dependent amyloid-β in cell models. |
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| SR-1277
SR-1277 is a potent, selective and ATP-competitive CK1δ/ε inhibitor with IC50 values of 49 nM and 260 nM, respectively.In addition, SR-1277 inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. 1340 nM, 311 nM and 109 nM, respectively, and can be used in cancer research. |
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