Catalog No.S8005 Synonyms: TCS PIM-1 4a

For research use only.

SMI-4a (TCS PIM-1 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.

SMI-4a Chemical Structure

CAS No. 438190-29-5

Selleck's SMI-4a has been cited by 8 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description SMI-4a (TCS PIM-1 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.
Pim1 [1]
(Cell-free assay)
17 nM
In vitro

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.[1] 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. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human PC3 cells Mk\LVJJwdGmoZYLheIlwdiCjc4PhfS=> M3jHUlQ5KGh? M2W1WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGOgZZN{[XluIFnDOVA:OTdizszN NWn1V5NDOTlyN{K2OVI>
DLD-1 cell NELweZZHfW6ldHnvckBie3OjeR?= NEfjNnc6PiCq MmDhTY5pcWKrdHnvckBw\iCpcn;3eIghd2ZiRFzEMVEh[2WubDDsbY5mKGGodHXyJFk3KGixdYLzJI9nKGW6cH;zeZJmKHSrbXWge4l1cCC2aHWgZ49ueG:3bnSg[Il{e2:udnXkJIlvKESPU1:sJGlEPTB;MUeuPEDPxE1? M{TpTVE2QTl|NUm0
HT-29 cell NWO1Z4ZMTnWwY4Tpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGe{b4f0bEBw\iCKVD2yPUBk\WyuIHzpcoUh[W[2ZYKgO|IsPzJiaH;1dpMhd2ZiZYjwc5N2emVidHnt[UB4cXSqIITo[UBkd22yb4Xu[EBlcXO|b3z2[YQhcW5iRF3TU{whUUN3ME2zNU41KM7:TR?= NInCcIQyPTl7M{W5OC=>
HCT116 cell NXPVbJFNTnWwY4Tpc44h[XO|YYm= MlzQO|IhcA>? M2juXGlvcGmkaYTpc44hd2ZiZ4Lve5RpKG:oIFjDWFEyPiClZXzsJIxqdmViYX\0[ZIhPzJiaH;1dpMhd2ZiZYjwc5N2emVidHnt[UB4cXSqIITo[UBkd22yb4Xu[EBlcXO|b3z2[YQhcW5iRF3TU{whUUN3ME20PE45KM7:TR?= NHq2ToEyPTl7M{W5OC=>
HEK293T cells Mn3kSpVv[3Srb36gZZN{[Xl? NWHxXWIzOC53IN88US=> MlHaNUBp MmfrTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCIbHHnMXBqdTFiYYX0c5Bpd3OyaH;yfYxifGmxbjDlfJBz\XO|ZXSgbY4hUEWNMkmzWEBk\WyuczDsZYJmdGWmIIfpeIghYzN{UF:0YUBifCByLkWgeW0h[W[2ZYKgNYhzKGK7IGfld5Rmem5iYnzveJRqdmd? NWrRXVdEOTlyN{K2OVI>
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. [2]

Protocol (from reference)

Animal Research:[2]
  • Animal Models: Nu/nu nude mice injected with pre-T-LBL cells
  • Dosages: 60 mg/Kg
  • Administration: p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 273.23


CAS No. 438190-29-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CC(=C1)C(F)(F)F)C=C2C(=O)NC(=O)S2

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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