Home JAK/STAT Pim inhibitor SMI-4a For research use only.

SMI-4a

Synonyms: TCS PIM-1 4a

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

SMI-4a Chemical Structure

CAS No. 438190-29-5

Purity & Quality Control

SMI-4a Related Products

Signaling Pathway

Pim Signaling Pathways

Pim Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human PC3 cells Proliferation assay 48 h Antiproliferative activity against human PC3 cells after 48 hrs by MTS assay, IC50=17 μM 19072652
DLD-1 cell Function assay 96 h Inhibition of growth of DLD-1 cell line after 96 hours of exposure time with the compound dissolved in DMSO, IC50=17.8 μM 15993594
HT-29 cell Function assay Inhibition of growth of HT-29 cell line after 72+72 hours of exposure time with the compound dissolved in DMSO, IC50=31.4 μM 15993594
HCT116 cell Function assay 72 h Inhibition of growth of HCT116 cell line after 72 hours of exposure time with the compound dissolved in DMSO, IC50=48.8 μM 15993594
HEK293T cells Function assay 0.5 μM 1 h Inhibition of human recombinant Flag-Pim1 autophosphorylation expressed in HEK293T cells labeled with [32PO4] at 0.5 uM after 1hr by Western blotting 19072652
Click to View More Cell Line Experimental Data

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.
Targets
Pim1 [1]
(Cell-free assay)
17 nM
In vitro
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]
In Vivo
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]
Animal Research Animal Models Nu/nu nude mice injected with pre-T-LBL cells
Dosages 60 mg/Kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 273.23 Formula

C11H6F3NO2S
CAS No. 438190-29-5 SDF Download SMI-4a SDF
Smiles C1=CC(=CC(=C1)C(F)(F)F)C=C2C(=O)NC(=O)S2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 55 mg/mL ( (201.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 55 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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