2. Metabolic Enzyme/Protease Apoptosis
  3. Pyruvate Kinase Apoptosis
  4. PKM2-IN-6

PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer.

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PKM2-IN-6 Chemical Structure

PKM2-IN-6 Chemical Structure

CAS No. : 771467-00-6

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PKM2-IN-6 Related Antibodies

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Description

PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer[1].

IC50 & Target

IC50: 23 nM (PKM2)[1]
In Vitro

PKM2-IN-6 (compound 7d) (0, 20, 40, 60, 80, 100 μM; 48 h) shows cytotoxicity with IC50s of 18.33, 47.00, 19.80 µM for COLO-205, A-549, MCF-7 cells, respectively[1].
PKM2-IN-6 (14.38 μM; 48 h) induces apoptosis and cell cycle arrest at G2 phase[1].
PKM2-IN-6 (14.38 μM; 24 h) reduces the PKM1 and PKM2 at the mRNA level[1].

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

PKM2-IN-6 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: COLO-205, A-549, MCF-7 cells
Concentration: 0, 20, 40, 60, 80, 100 μM
Incubation Time: 48 h
Result: Showed cell cytotoxicity with IC50s of 18.33, 47.00, 19.80 µM for COLO-205, A-549, MCF-7 cells, respectively.

RT-PCR[1]

Cell Line: 4T1 cells
Concentration: 14.38 μM
Incubation Time: 24 h
Result: Significantly reduced the level of PKM1 and PKM2 at the mRNA level.

Apoptosis Analysis[1]

Cell Line: 4T1 cells
Concentration: 14.38 μM
Incubation Time: 48 h
Result: Induced apoptosis the percentage of live cells depreciated from 82.64% in control to 5.44% and the percentage of late apoptotic cells was 50.32% and necrotic cells were 44.08% in 2D culture; the difference is diminished as 89.05% of live cells in control dropped down to 52.45% and the percentage of late apoptotic cells was lesser (only 9.84%) and necrotic cells were 36.62% in 3D cell culture.
In Vivo

PKM2-IN-6 (25, 50 mg/kg; p.o.; daily for 3 weeks) decreases the tumor volume and tumor weight in mice[1].

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

Animal Model: 6-8 weeks, Female CD-1 nude mice (4T1-Red-FLuc cells)[1]
Dosage: 25, 50 mg/kg
Administration: P.o.; daily for 3 weeks
Result: Showed a significant regression in tumor volume and rendered significant reduction in tumor weight.
Molecular Weight

322.38

Formula

C17H14N4OS
CAS No.
SMILES

COC1=CC=CC=C1NC2=NC(C3=CN=C4C=CC=CN43)=CS2
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Purity & Documentation
References
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PKM2-IN-6 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKM2-IN-6771467-00-6Pyruvate KinaseApoptosisG2 phase4T1 cellsanticancerbreast cancerPKM1PKM2Inhibitorinhibitorinhibit

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