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PKM2 inhibitor(compound 3k)

Synonyms: PKM2-IN-1

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

PKM2 inhibitor(compound 3k) Chemical Structure

CAS No. 94164-88-2

Purity & Quality Control

PKM2 inhibitor(compound 3k) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay, IC50=0.18μM 28688274
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells after 48 hrs by MTS assay, IC50=0.29μM 28688274
NCI-H1299 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H1299 cells after 48 hrs by MTS assay, IC50=1.56μM 28688274
NCI-H1299 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H1299 cells after 48 hrs in presence of PKM2 activator FBP by MTS assay, IC50=2.01μM 28688274
BEAS2B Cytotoxicity assay 48 hrs Cytotoxicity against human BEAS2B cells assessed as reduction in cell viability after 48 hrs by MTS assay, IC50=18.46μM 28688274
Click to View More Cell Line Experimental Data

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
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 Research 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.
In Vivo
In vivo

Compound 3K (PKM2-IN-1) is an enzymatic inhibitor of pyruvate kinase M2 (PKM2).
Animal Research Animal Models Male C57BL/6 mice
Dosages 1.2 μM
Administration Topical

Chemical Information & Solubility

Molecular Weight 345.48 Formula

C18H19NO2S2
CAS No. 94164-88-2 SDF Download PKM2 inhibitor(compound 3k) SDF
Smiles CC1=C(C(=O)C2=CC=CC=C2C1=O)CSC(=S)N3CCCCC3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6 mg/mL ( (17.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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