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.
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- 화학식: C20H15FN2OS
- 분자량:350.41
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
More
Biological Activity
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DNA Polymerase |
PKM2 |
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.
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.
Chemical Information
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분자량 350.41
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- 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