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Art. -Nr.: HY-181930

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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. Nr.: 3112758-72-9
Formel: C₂₈H₂₇N₅O₂
Molecular Weight:465.55

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Please store the product under the recommended conditions in the Certificate of Analysis.

TNIK-IN-10 Chemical Structure

CAS. Nr.: 3112758-72-9

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Beschreibung

Alle Wnt Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

HCT116 human colorectal cancer cells
Concentration:

1.9-15 μM
Incubation Time:

48 h
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.

In Vivo

TNIK-IN-10 (30-50 mg/kg; i.p.; 5 consecutive days followed by 2 days off, for a total of 16 days) potently and dose-dependently inhibits the growth of HCT116 xenografts in BALB/c nude mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (male, 6 weeks old, 19-22 g, subcutaneous xenograft)^[1]
Dosage:

30 mg/kg; 50 mg/kg
Administration:

i.p.; 5-days-on/2-days-off; 16 days
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

CAS. Nr. 3112758-72-9
Molecular Weight 465.55
Formel C₂₈H₂₇N₅O₂
SMILES

CC(C)NCCN(CCO1)C(C(C1=C2)=CC=C2C3=CN=C(NC=C4C5=CC(C#N)=CC=C5)C4=C3)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Niu X, et al. Discovery of potent TNIK inhibitors containing a 1H-pyrrolo [2, 3-b] pyridine scaffold as promising therapeutics for colorectal cancer[J]. European Journal of Medicinal Chemistry, 2026: 118717.

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Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

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Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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TNIK-IN-10

Alle Wnt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

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TNIK-IN-10 Related Classifications

HY-181930 Related Classifications