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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 |
| Related Pim Products |
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| SGI-1776
SGI-1776 is novel small molecule inhibitor of PIM kinase activity with IC50 of 7 ± 1.8, 363 ± 27.6 and 69 ± 9.2 nM for Pim-1, Pim-2, and Pim-3, respectively. |
| SMI-4a
SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modest potent to Pim-2, does not significantly inhibit other serine/threonine- or tyrosine-kinases. |
| CX-6258
CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity. |
| Hispidulin
Hispidulin is a natural flavonoid with a wide range of biological activities. Hispidulin is an inhibitor of PIM-1 with IC50 value of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. |
| AZD-1208
AZD1208 is a potent, highly selective, and orally available Pim kinase inhibitor that effectively inhibits all three isoforms at <5 nM or <150 nM in enzyme and cell assays, respectively. |
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