PKM2 inhibitor(compound 3k)

Catalog No.S8616 Batch:S861601

Technical Data

Formula

C₁₈H₁₉NO₂S₂

Molecular Weight

345.48

CAS No.

94164-88-2

Solubility (25°C)*

In vitro

DMSO

6 mg/mL (17.36 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45%ddH2O	0.5mg/ml	Taking the 1 mL working solution as an example, add 100 μL of 5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95%Corn oil	0.25mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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].

In vivo

Compound 3K (PKM2-IN-1) is an enzymatic inhibitor of pyruvate kinase M2 (PKM2).

Protocol (from reference)

Cell Assay:^{^[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.
Animal Study:^{^[2]}	Animal Models Male C57BL/6 mice Dosages 1.2 μM Administration Topical

Cell Assay:^{^[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.

Animal Study:^{^[2]}

Animal Models
Male C57BL/6 mice
Dosages
1.2 μM
Administration
Topical

References

Selleck's PKM2 inhibitor(compound 3k) has been cited by 28 publications

Context-dependent modification of PFKFB3 in hematopoietic stem cells promotes anaerobic glycolysis and ensures stress hematopoiesis [ Elife, 2024, 12RP87674]	PubMed: 38573813
Transcriptomics of Hirschsprung disease patient-derived enteric neural crest cells reveals a role for oxidative phosphorylation [ Nat Commun, 2023, 14(1):2157]	PubMed: 37061531
Mediation of PKM2-dependent glycolytic and non-glycolytic pathways by ENO2 in head and neck cancer development [ J Exp Clin Cancer Res, 2023, 42(1):1]	PubMed: 36588153
USP11 exacerbates neuronal apoptosis after traumatic brain injury via PKM2-mediated PI3K/AKT signaling pathway [ Brain Res, 2023, 1807:148321]	PubMed: 36898475
Microglial hexokinase 2 deficiency increases ATP generation through lipid metabolism leading to β-amyloid clearance [ Nat Metab, 2022, 4(10):1287-1305]	PubMed: 36203054
Long non-coding RNA VAL facilitates PKM2 enzymatic activity to promote glycolysis and malignancy of gastric cancer [ Clin Transl Med, 2022, 12(10):e1088]	PubMed: 36229913
Lactylation of PKM2 Suppresses Inflammatory Metabolic Adaptation in Pro-inflammatory Macrophages [ Int J Biol Sci, 2022, 18(16):6210-6225]	PubMed: 36439872
Novel Specific Pyruvate Kinase M2 Inhibitor, Compound 3h, Induces Apoptosis and Autophagy through Suppressing Akt/mTOR Signaling Pathway in LNCaP Cells [ Cancers (Basel), 2022, 15(1)265]	PubMed: 36612260
Inhibition of abnormally activated HIF-1α-GLUT1/3-glycolysis pathway enhances the sensitivity of hepatocellular carcinoma to 5-caffeoylquinic acid and its derivatives [ Eur J Pharmacol, 2022, S0014-2999(22)00105-4]	PubMed: 35189090
PDGF-BB/PDGFRβ promotes epithelial-mesenchymal transition by affecting PI3K/AKT/mTOR-driven aerobic glycolysis in Wilms' tumor G401 cells [ Cell Biol Int, 2022, 10.1002/cbin.11780]	PubMed: 35165984

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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