1. MAPK/ERK Pathway
    Stem Cell/Wnt
    Apoptosis
  2. MAP4K
    Wnt
    Apoptosis
  3. KY-05009

KY-05009 

Cat. No.: HY-124745
Handling Instructions

KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.

For research use only. We do not sell to patients.

KY-05009 Chemical Structure

KY-05009 Chemical Structure

CAS No. : 1228280-29-2

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Description

KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity[1].

IC50 & Target[1]

TNIK

100 nM (Ki)

In Vitro

KY-05009 (0.1-30 μM; 24 hours; RPMI8226 cells) treatment inhibits the proliferation of RPMI8226 cells in a dose-dependent manner[1].
KY-05009 (1-3 μM; 48-72 hours; RPMI8226 cells) treatment induces caspase-dependent apoptosis in RPMI8226 cells in a dose-dependent manner[1].
KY-05009 (3 μM; 1 hour; RPMI8226 cells) treatment suppresses the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4[1].
. KY-05009 (3 μM; 9 hours; RPMI8226 cells) treatment inhibits the IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4[1].

Cell Proliferation Assay[1]

Cell Line: RPMI8226 cells
Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of RPMI8226 cells.

Apoptosis Analysis[1]

Cell Line: RPMI8226 cells
Concentration: 1 μM, 3 μM, 10 μM
Incubation Time: 48 hours, 72 hours
Result: Induced the binding of fluorescent Annexin V and 7-amino-actinomycin D (7-AAD) uptake.

RT-PCR[1]

Cell Line: RPMI8226 cells
Concentration: 3 μM
Incubation Time: 1 hour
Result: Suppressed the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4.

Western Blot Analysis[1]

Cell Line: RPMI8226 cells
Concentration: 3 μM
Incubation Time: 9 hours
Result: The IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4 were inhibited.
Molecular Weight

352.41

Formula

C₁₈H₁₆N₄O₂S

CAS No.

1228280-29-2

SMILES

O=C(C1=C(NC(C2=CC=C(C)C=C2)=O)SC(NC3=CC=CC=C3)=N1)N

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

KY-05009KY05009KY 05009MAP4KWntApoptosisMAPK Kinase Kinase KinaseTNIKIL-6plasma-cellssmyelomaanti-proliferativecaspase-dependentapoptosisanti-canceraminothiazoleInhibitorinhibitorinhibit

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