2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. DNA/RNA Synthesis Pyruvate Kinase
  4. 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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Multi-target kinase-IN-9

Multi-target kinase-IN-9 Chemical Structure

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Multi-target kinase-IN-9 Related Antibodies

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Description

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[1].

IC50 & Target

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.

Multi-target kinase-IN-9 Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2 hepatocellular carcinoma cells
Concentration: 3.12-100 μM
Incubation Time: 48 h
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 (compound 2c) (23 μM; local administration; single dose) significantly inhibits hepatocellular carcinoma tumor growth in the chick embryo chorioallantoic membrane (CAM) model, reducing the average tumor volume to 65% of the baseline level within 48 h of treatment at the IC50 dose[1].
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.

Animal Model: ROSS308 fertilized eggs[1]
Dosage: 10-1000 μM
Administration: topical; single dose
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.
Molecular Weight

350.41

Formula

C20H15FN2OS
SMILES

FC(C=C1)=CC=C1SC2=CC=C(/C=N/NC(C3=CC=CC=C3)=O)C=C2
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
References
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Multi-target kinase-IN-9 Related Classifications

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Help & FAQs
  • 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:

Multi-target kinase-IN-9DNA/RNA SynthesisPyruvate KinaseDNA ligase 1DNA polymerase betamethyl-CpG binding protein 2tyrosyl-DNA phosphodiesterase 1aldehyde dehydrogenase 1A1pyruvate kinase M2hepatocellular carcinoma cellslysosomal alpha-glucosidaseanti-silencing function 1A histone chaperoneATP-dependent DNA helicase Q1Inhibitorinhibitorinhibit

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