For research use only.

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

8 publications

SMI-4a Chemical Structure

CAS No. 438190-29-5

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.

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

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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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 MoLwVJJwdGmoZYLheIlwdiCjc4PhfS=> NVPvXHdDPDhiaB?= NYrUZlZUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1zNzFOwG0> Mm\jNVkxPzJ4NUK=
DLD-1 cell M1PFcmZ2dmO2aX;uJIF{e2G7 NV;PZpI4QTZiaB?= M1vRc2lvcGmkaYTpc44hd2ZiZ4Lve5RpKG:oIFTMSE0yKGOnbHygcIlv\SCjZoTldkA6PiCqb4Xyd{Bw\iCneIDvd5Vz\SC2aX3lJJdqfGhidHjlJINwdXCxdX7kJIRqe3OxbI\l[EBqdiCGTWPPMEBKSzVyPUG3Mlgh|ryP NFm3cVEyPTl7M{W5OC=>
HT-29 cell MW\GeY5kfGmxbjDhd5NigQ>? Mn3FTY5pcWKrdHnvckBw\iCpcn;3eIghd2ZiSGStNlkh[2WubDDsbY5mKGGodHXyJFczMzd{IHjveZJ{KG:oIHX4dI9{fXKnIITpcYUhf2m2aDD0bIUh[2:vcH;1coQh\Gm|c3;seoVlKGmwIFTNV28tKEmFNUC9N|EvPCEQvF2= MlTmNVU6QTN3OUS=
HCT116 cell MmLRSpVv[3Srb36gZZN{[Xl? MWG3NkBp NEn1R2tKdmirYnn0bY9vKG:oIHfyc5d1cCCxZjDIR3QyOTZiY3XscEBtcW6nIHHmeIVzKDd{IHjveZJ{KG:oIHX4dI9{fXKnIITpcYUhf2m2aDD0bIUh[2:vcH;1coQh\Gm|c3;seoVlKGmwIFTNV28tKEmFNUC9OFgvQCEQvF2= NYLEfpdjOTV7OUO1PVQ>
HEK293T cells MYnGeY5kfGmxbjDhd5NigQ>? M{LxSVAvPSEQvF2= NFrtV2UyKGh? NFjnflJKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IF\sZYcuWGmvMTDheZRweGixc4Doc5J6dGG2aX;uJIV5eHKnc4Pl[EBqdiCKRVuyPVNVKGOnbHzzJIxi[mWuZXSge4l1cCCdM{LQU|ReKGG2IECuOUB2VSCjZoTldkAycHJiYomgW4V{fGW{bjDicI91fGmwZx?= M2L6S|E6ODd{NkWy

... Click to View More Cell Line Experimental Data

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

Solubility (25°C)

In vitro DMSO 55 mg/mL (201.29 mM)
Ethanol 32 mg/mL (117.11 mM)
Water Insoluble
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

* 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.

Chemical Information

Molecular Weight 273.23


CAS No. 438190-29-5
Storage powder
in solvent
Synonyms TCS PIM-1 4a
Smiles C1=CC(=CC(=C1)C(F)(F)F)C=C2C(=O)NC(=O)S2

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Pim Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID