TCS PIM-1 1 is a potent, ATP-competitive inhibitor of Pim-1 kinase. This compound displays selectivity over Pim-2 and MEK1/MEK2 (IC50 values are 50, >20000 and >20000 nM for Pim-1, Pim-2, and MEK1/MEK2, respectively). TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism.
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Source | Cancer Lett (2012). Figure 2. TCS PIM-1 1 |
| Method | Effect of Pim-1 on microtubule formation | |
| Cell Lines | PC-3 cells | |
| Concentrations | - | |
| Incubation Time | 18 h | |
| Results | The knockdown of Pim-1 did not modify the effect of these agents on tubulin polymerizing activity, indicating that the induction and potentiation of apoptosis in Pim-1 knock- down cells were not relevant to tubulin dynamics when exposed to these agents. |
| Molecular Weight | 367.2 |
| Formula | C18H11BrN2O2 |
| CAS Number | 491871-58-0 |
| Solubility (25°C) | DMSO 100 mM |
| 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 Pim Products |
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| R8-T198wt
R8-T198wt is a cell-permeable carboxyl-terminal p27Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase. |
| FD1024
FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). |
| Pim-1 kinase inhibitor 5
Pim-1 kinase inhibitor 5 is a Pim-1 kinase inhibitor (IC50: 0.61 μM). |
| Pim-1 kinase inhibitor 4
Pim-1 kinase inhibitor 4 is a Pim-1 kinase inhibitor (IC50: 17.01 nM). |
| Pim-1 kinase inhibitor 6
Pim-1 kinase inhibitor 6 is a potent Pim-1 kinase inhibitor with IC50 value of 0.46 μM, and has significant cytotoxic effect on cancer cells. |
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