Catalog No.S8005 Synonyms: TCS PIM-1 4a
Molecular Weight(MW): 273.23
SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.
1 Customer Review
Loss of proliferation in ATL-derived cell lines by the Pim-kinase inhibitors, Smi-4a (C). Cell counts were repeated at least twice. Results represent the percentage of cells alive after 5 days of Pim inhibitor treatment, compared with 5 days treated with DMSO. For Smi-4a treatment, cells were treated with 0, 10, or 20 μM Smi-4a. Normal PBMCs (n = 2) were used as a control. Western blots indicate loss of Pim1 targets, p-4EBP1 (Thr37/46), p-p70S6K (Thr389), and loss of pBad (Ser20) (negligible for Smi-4a) after 24 hours with 0, 10, 20, or 40 μM Smi-4a or DMSO control.
Blood, 2016, 127:2439-2450.. SMI-4a purchased from Selleck.
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|Description||SMI-4a is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.|
|Features||SMI-4a (5μM) synergizes with rapamycin (5 nM) to cause significant growth inhibition of leukemic cells.|
SMI-4a is an ATP competitive inhibitor of Pim1 with IC50 of 17 nM. SMI-4a shows high selectivity for Pim1 against a panel of kinases. SMI-4a inhibits the in vitro phosphorylation by Pim-1 of the known substrate, the translational repressor 4E-BP1. SMI-4a (5μM) inhibits pancreatic and leukemic cells growth. SMI-4a reduces phosphorylation of the Pim target Bad in prostate and hematopoietic cells. SMI-4a causes cell cycle arrest and reverses the antiapoptotic activity of Pim-1. SMI-4a increases the amount of p27Kip1 in the nucleus. SMI-4a treatment of pre-T-LBL inhibits the mTOR pathway. SMI-4a reduces MYC protein expression in pre-T-LBL. SMI-4a treatment induces up-regulation of MAPK pathway. 
|In vivo||SMI-4a (60 mg/Kg) treatment twice daily significantly reduce tumor size and is well tolerated. Tumors harvested 1 hour after the final oral gavage of SMI-4a demonstrates decreased phosphorylation of p70 S6K compared with tumors from mice treated with vehicle, whereas in comparison total p70 S6K expression isunchanged. |
|In vitro||DMSO||55 mg/mL (201.29 mM)|
|Ethanol||32 mg/mL (117.11 mM)|
|In vivo||Add solvents to the product individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||TCS PIM-1 4a|
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