TNIK-IN-10
TNIK-IN-10 (Compound N15) is a TNIK inhibitor with an IC50 of 0.49 nM against human TNIK. TNIK-IN-10 inhibits the enzymatic activity of TNIK, downregulates the expression of Wnt pathway target genes c-Myc and AXIN2, and reduces the protein expression of LRP5 and LRP6. TNIK-IN-10 induces apoptosis. TNIK-IN-10 exhibits anticancer activity against colorectal cancer. TNIK-IN-10 can be used in the research of colorectal cancer.
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- CAS No.: 3112758-72-9
- Formule: C28H27N5O2
- Masse moléculaire:465.55
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
TNIK-IN-10 (range of concentrations; 60 min) potently inhibits recombinant human TNIK enzymatic activity with an IC50 of 0.49 nM[1].
TNIK-IN-10 shows high metabolic stability in human liver microsomes with a half-life of 241 min[1].
TNIK-IN-10 (72 h) potently inhibits HCT116 human colorectal cancer cell proliferation with an IC50 of 2.24 ± 0.87 μM[1].
TNIK-IN-10 (1.9-7.5 μM; 72 h) dose-dependently induces apoptosis in HCT116 colorectal cancer cells after 72 h of treatment[1].
TNIK-IN-10 (1.9-7.5 μM; 72 h) alters cell cycle progression in HCT116 human colorectal cancer cells after 72 h of treatment, reducing the G1-phase population and increasing the S-phase population[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 human colorectal cancer cells
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Concentration:1.9-15 μM
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Incubation Time:48 h
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Result:Reduced protein expression of Wnt target genes c-Myc and AXIN2, and downregulated LRP5 and LRP6 protein levels in a dose-dependent manner; TNIK protein expression remained unchanged.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6 weeks old, 19-22 g, subcutaneous xenograft)[1]
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Dosage:30 mg/kg; 50 mg/kg
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Administration:i.p.; 5-days-on/2-days-off; 16 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 69.6% at 50 mg/kg.
Markedly reduced tumor weights in both 30 mg/kg and 50 mg/kg treatment groups.
Induced transient body weight reductions early in treatment, which subsequently stabilized.
Chemical Information
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CAS No. 3112758-72-9
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Masse moléculaire 465.55
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Formule C28H27N5O2
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SMILES
CC(C)NCCN(CCO1)C(C(C1=C2)=CC=C2C3=CN=C(NC=C4C5=CC(C#N)=CC=C5)C4=C3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TNIK-IN-10 Related Classifications
HY-181930 Related Classifications
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