Multi-target kinase-IN-9
Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research.
For research use only. We do not sell to patients.
- Formula: C20H15FN2OS
- Molecular Weight:350.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
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Biological Activity
Description
IC50 & Target
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DNA Polymerase |
PKM2 |
In Vitro
Multi-target kinase-IN-9 (compound 2c) (3.12-100 μM; 48 h) exerts dose-dependent antiproliferative effects on HepG2 hepatocellular carcinoma cells, with an IC50 of 23 μM and a GI50 of 6.25 μM after 48 h of treatment[1].
Multi-target kinase-IN-9 binds to PKM2 with a Kd value of 5.7 μM[1].
Multi-target kinase-IN-9 binds to DNA in the MeCP2+DNA complex with high affinity (Kd=0.69 μM), and binds to free MeCP2 with moderate affinity (Kd=12.27 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 hepatocellular carcinoma cells
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Concentration:3.12-100 μM
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Incubation Time:48 h
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Result:Caused a moderate decrease in HepG2 cell growth at 3.12 μM.
Resulted in a nearly 40-50% reduction in cell viability at 6.25 μM and above.
Exhibited an IC50 of 23 μM and a GI50 of 6.25 μM.
In Vivo
Multi-target kinase-IN-9 (10-1000 μM; local administration) exhibits dose-dependent anti-angiogenic activity in the chick CAM model, with the strongest effect observed at the dose of 1000 μM, and the activity gradually decreases at lower doses and over time[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ROSS308 fertilized eggs[1]
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Dosage:10-1000 μM
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Administration:topical; single dose
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Result:Achieved a mean antiangiogenic score of around 1.5 at 24 h and around 1.0 at 48 h at 1000 μM.
Achieved a mean antiangiogenic score of around 1.0 at 24 h and 0.5 at 48 h at 100 μM.
Achieved a mean antiangiogenic score below 0.5 at 24 h, with no detectable activity (score 0) at 48 h at 10 μM.
- Human pluripotent stem cell endothelial-cell differentiation
- Mammalian live/dead viability and cytotoxicity staining
- Vascular/Branching Fractal Analysis
- Liver Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Cell Cytotoxicity Assay
- Autophagy
- Endothelial Tube Formation Assay
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Cell invasion
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Lysosome and acidic-vesicle live-cell staining
- Subcutaneous Cell-Line-Derived Xenograft
- hPSC maintenance and expansion
- Macroautophagy Solutions
- Orthotopic Cell-Line Xenograft
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Molecular Weight 350.41
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Formula C20H15FN2OS
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SMILES
FC(C=C1)=CC=C1SC2=CC=C(/C=N/NC(C3=CC=CC=C3)=O)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Multi-target kinase-IN-9
- DNA/RNA Synthesis
- Pyruvate Kinase
- DNA ligase 1
- DNA polymerase beta
- methyl-CpG binding protein 2
- tyrosyl-DNA phosphodiesterase 1
- aldehyde dehydrogenase 1A1
- pyruvate kinase M2
- hepatocellular carcinoma cells
- lysosomal alpha-glucosidase
- anti-silencing function 1A histone chaperone
- ATP-dependent DNA helicase Q1
- Inhibitor
- inhibitor
- inhibit