SMI-4a

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.
Targets
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 NX3odWxJWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUKxZpRqPDhiaB?= NGCwNVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDh[pRmeiB2ODDodpMh[nliTWTTJIF{e2G7LDDJR|UxRTF5IN88US=> MoDONVkxPzJ4NUK=
DLD-1 cell MlHlSpVv[3Srb36gZZN{[Xl? NY\5[nNXQTZiaB?= Mm\VTY5pcWKrdHnvckBw\iCpcn;3eIghd2ZiRFzEMVEh[2WubDDsbY5mKGGodHXyJFk3KGixdYLzJI9nKGW6cH;zeZJmKHSrbXWge4l1cCC2aHWgZ49ueG:3bnSg[Il{e2:udnXkJIlvKESPU1:sJGlEPTB;MUeuPEDPxE1? MVmxOVk6OzV7NB?=
HT-29 cell M1y5[mZ2dmO2aX;uJIF{e2G7 NWHCeFZPUW6qaXLpeIlwdiCxZjDndo94fGhib3[gTHQuOjliY3XscEBtcW6nIHHmeIVzKDd{K{eyJIhwfXK|IH;mJIV5eG:|dYLlJJRqdWVid3n0bEB1cGViY3;tdI92dmRiZHnzd49tfmWmIHnuJGROW09uIFnDOVA:OzFwNDFOwG0> NXn4U2pQOTV7OUO1PVQ>
HCT116 cell Mnf4SpVv[3Srb36gZZN{[Xl? M2rvblczKGh? NUDFXFF7UW6qaXLpeIlwdiCxZjDndo94fGhib3[gTGNVOTF4IHPlcIwhdGmwZTDh[pRmeiB5MjDoc5VzeyCxZjDlfJBwe3W{ZTD0bY1mKHerdHigeIhmKGOxbYDveY5lKGSrc4PvcJZm\CCrbjDEUXNQNCCLQ{WwQVQ5NjhizszN Mki1NVU6QTN3OUS=
HEK293T cells MWDGeY5kfGmxbjDhd5NigQ>? MUSwMlUh|ryP NXSz[Ww4OSCq NG\hfGJKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IF\sZYcuWGmvMTDheZRweGixc4Doc5J6dGG2aX;uJIV5eHKnc4Pl[EBqdiCKRVuyPVNVKGOnbHzzJIxi[mWuZXSge4l1cCCdM{LQU|ReKGG2IECuOUB2VSCjZoTldkAycHJiYomgW4V{fGW{bjDicI91fGmwZx?= NULR[Yh1OTlyN{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

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

Chemical Information

Molecular Weight 273.23
Formula

C11H6F3NO2S

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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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