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Cat. No.: HY-129165

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ZINC08383544

ZINC08383544 is a PKM2 activator with anti-tumor activity. ZINC08383544 binds to the dimer-dimer interface of PKM2, promotes tetramer formation, blocks nuclear translocation, inhibits the expression of glycolysis-related genes such as GLUT1, and reduces T cell-mediated inflammatory responses. ZINC08383544 can be used in cancer-related research such as cervical cancer.

For research use only. We do not sell to patients.

CAS No.: 618361-63-0
Formula: C₃₀H₃₀N₂O₆
Molecular Weight:514.58

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

ZINC08383544 Chemical Structure

CAS No.: 618361-63-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

PKM2

GLUT1

All GLUT Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC50	<100 nM	Inhibition of cell viability against human HeLa cancer cells assessed by CCK-8 assay. Inhibition of cell viability against human HeLa cancer cells assessed by CCK-8 assay.	30133040
HCT-116	IC50	<100 nM	Inhibition of cell viability against human HCT116 cancer cells assessed by CCK-8 assay. Inhibition of cell viability against human HCT116 cancer cells assessed by CCK-8 assay.	30133040

In Vitro

Carbohydrate MetabolismAnti-cancer

Carbohydrate Metabolism

ZINC08383544 forms a stable complex with dimeric human PKM2, with a binding free energy of -84.285 kJ/mol; it promotes the formation of tetramers from purified human PKM2; and it activates purified human PKM2 in a dose-dependent manner, increasing its activity from 6.5 U/mL to a maximum of 9.63 U/mL at 300 nM^[1].
ZINC08383544 (200 nM) blocks the nuclear translocation of PKM2, increases cytoplasmic PKM2 levels, and reduces the phosphorylation levels of nuclear histone H3-T11 and STAT3-Y705 in HeLa and HepG2 cells^[1].
ZINC08383544 (25-200 nM) dose-dependently downregulates the expression of LDHA and GLUT1 in HeLa and HepG2 cells, with a stronger effect on LDHA in HeLa cells^[1].

Anti-cancer

ZINC08383544 inhibits the viability of HeLa, HCT116, SKBR3, HepG2 and H1299 cancer cells in a dose-dependent manner (with IC₅₀ < 100 nM for HeLa and HCT116 cells), while exerting no significant effect on normal LO2 hepatocytes^[1].

Anti-cancer

Carbohydrate Metabolism

ZINC08383544 (100-600 nM; 24 h) exerts antiproliferative effects on HeLa and HepG2 cells, and these effects depend on the expression of PKM2, since knockdown of PKM2 significantly reduces the inhibitory activity of this compound^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

HeLa, HepG2 (PKM2 siRNA-transfected)
Concentration:

0, 100, 200, 3000, 400, 500, 600 nM
Incubation Time:

24 h (siRNA incubation); 24 h (compound incubation)
Result:

Reduced PKM2 expression to less than 15% of normal levels in both cell lines via PKM2-targeting siRNA.
Significantly relieved the inhibitory effect on HeLa and HepG2 cell viability following PKM2 knockdown.

Related Protocols :

Chemical Information

CAS No. 618361-63-0
Molecular Weight 514.58
Formula C₃₀H₃₀N₂O₆
SMILES

O=C(C1=CC=C2OCCOC2=C1)C3=C(O)C(=O)N(CC=4C=NC=CC4)C3C5=CC=C(OCCCCC)C=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Li Y, et al. Computer-aided identification of a novel pyruvate kinase M2 activator compound. Cell proliferation. 2018 Dec;51(6):e12509.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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