PKM2-IN-12
PKM2-IN-12 is an orally active PKM2 inhibitor with an IC50 of 10 nM. PKM2-IN-12 inhibits COLO-205 cell proliferation and migration, arrests the cell cycle, and induces apoptosis. PKM2-IN-12 significantly reduces cellular levels of lactate, pyruvate, and ROS. PKM2-IN-12 directly kills cancer cells and restores disrupted gut microbiota balance in mice model. PKM2-IN-12 can be used to study colorectal cancer.
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- Formel: C23H14Cl2N4OS
- Molecular Weight:465.35
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PKM2 10 nM (IC50) |
In Vitro
PKM2-IN-12 (Compound 10j) (24 h) shows significant differences in sensitivity in COLO-205, CAL-27 and MCF-7 cells with IC50s of 4.21, 13.3 and 22.34 μM[1].
PKM2-IN-12 (4.21 μM, 48 h) mainly kills COLO-205 cells by inducing late apoptosis and blocks the cells at the G2 phase[1].
PKM2-IN-12 (4.21 μM) significantly inhibits the migration ability of COLO-205 cells[1].
PKM2-IN-12 (4.21 μM, 0-48 h) significantly reduces the levels of lactate, pyruvate and ROS within the COLO-205 cells[1].
PKM2-IN-12 (4.21 μM, 48 h) increases the expression of PKM2 monomers and tetramers, but did not affect PKM1 in COLO-205 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AOM (HY-111375)/DSS (HY-116282C)-induced colitis-associated colorectal cancer (CAC) model established in BALB/c mice[1]
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Dosage:50, 75 and 100 mg/kg
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Administration:Oral administration (p.o,), once every three days for 72 days
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Result:Significantly inhibited tumor formation and reduce tumor burden.
Increased the length of the colon, and maintain the stable weight of the mice.
Significantly restored the alpha diversity of the intestinal microbiota in mice.
Reduced the pathological scores of the colon tissue, including inflammatory cell infiltration, epithelial damage and abnormal glandular structure.
Chemical Information
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Molecular Weight 465.35
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Formel C23H14Cl2N4OS
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SMILES
O=C(C1=C(C2=CC=C(Cl)C=C2)N=C(NC3=CC=C(Cl)C=C3)S1)C4=CN=C5C=CC=CN54
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PKM2-IN-12 Related Classifications
HY-178748 Related Classifications
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