PKM2 inhibitor(compound 3k)

Catalog No.S8616 Synonyms: PKM2-IN-1

For research use only.

PKM2 inhibitor(Compound 3K, PKM2-IN-1) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2.

PKM2 inhibitor(compound 3k) Chemical Structure

CAS No. 94164-88-2

Selleck's PKM2 inhibitor(compound 3k) has been cited by 18 publications

Purity & Quality Control

Choose Selective PKM Inhibitors

Biological Activity

Description PKM2 inhibitor(Compound 3K, PKM2-IN-1) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2.
Targets
PKM2 [1]
(Cell-free assay)
2.95 μM
In vitro

The well performing compound 3k shows nanomolar antiproliferative activity toward a series of cancer cell lines with high expression of PKM2 including HCT116, Hela and H1299 with IC50 values ranging from 0.18-1.56 μM. Moreover, compound 3k exhibits more cytotoxicity on cancer cells than normal cells[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 M{npOGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Ml;aOFghcHK| MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTTJIF{e2G7LDDJR|UxRTBwMUlOwG0> NWnkcXZwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PFgzPzRpPkK4Olg5Ojd2PD;hQi=>
HeLa M3y2O2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M3f0VFQ5KGi{cx?= M3u3bGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXMZUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTTJIF{e2G7LDDJR|UxRTBwMkpOwG0> NWnPWFFVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PFgzPzRpPkK4Olg5Ojd2PD;hQi=>
NCI-H1299 M3OybGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVO0PEBpenN? MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INVI6QSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRUKGG|c3H5MEBKSzVyPUGuOVbPxE1? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ6OEK3OEc,Ojh4OEiyO|Q9N2F-
NCI-H1299 MmHnRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MlLyOFghcHK| NVvPb2QySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF{OUmgZ4VtdHNiYX\0[ZIhPDhiaILzJIlvKHC{ZYPlcoNmKG:oIGDLUVIh[WO2aY\heI9zKE[EUDDifUBOXFNiYYPzZZktKEmFNUC9Nk4xOc7:TR?= NGTzN|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[4PFI4PCd-Mki2PFgzPzR:L3G+
BEAS2B NFH3ZXFEgXSxdH;4bYNqfHliYYPzZZk> MoT2OFghcHK| NFG0XFdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDTUGVMlKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDNWHMh[XO|YYmsJGlEPTB;MUiuOFbPxE1? MknlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OEiyO|QoRjJ6Nki4Nlc1RC:jPh?=

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HCT116, Hela, H1299, BEAS-2B
  • Concentrations: 0.078, 0.156, 0.313, 0.625 μM
  • Incubation Time: 48 h
  • Method:

    Cell viability is detected with the MTS assay. Briefly, 5000 cells in per well are plated in 96-well plates. After incubated for 12 h, the cells are treated with different concentration of tested compound or DMSO (as negative control) for 48 h. Then 20 μL MTS is added in per well and incubated at 37°C for 3h. Absorbance of each well is determined by a microplate reader at a 490 nm wavelength. The IC50 values are calculated using Prism Graphpad software of the triplicate experiment.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 345.48
Formula

C18H19NO2S2

CAS No. 94164-88-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=O)C2=CC=CC=C2C1=O)CSC(=S)N3CCCCC3

In vivo Formulation Calculator (Clear solution)

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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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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.

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