KY-05009

Modify Date: 2024-01-06 18:44:23

KY-05009 Structure
KY-05009 structure
Common Name KY-05009
CAS Number 1228280-29-2 Molecular Weight 352.410
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C18H16N4O2S Melting Point N/A
MSDS USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of KY-05009


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].

 Names

Name 2-Anilino-5-[(4-methylbenzoyl)amino]-1,3-thiazole-4-carboxamide
Synonym More Synonyms

 KY-05009 Biological Activity

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].
Related Catalog
Target

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.
References

[1]. Lee Y, et al. Synergistic inhibition effect of TNIK inhibitor KY-05009 and receptor tyrosine kinase inhibitor dovitinib on IL-6-induced proliferation and Wnt signaling pathway in human multiple myeloma cells. Oncotarget. 2017 Jun 20;8(25):41091-41101.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C18H16N4O2S
Molecular Weight 352.410
Exact Mass 352.099396
LogP 2.83
Index of Refraction 1.728

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
RIDADR NONH for all modes of transport

 Synonyms

MFCD29059915
4-Thiazolecarboxamide, 5-[(4-methylbenzoyl)amino]-2-(phenylamino)-
2-Anilino-5-[(4-methylbenzoyl)amino]-1,3-thiazole-4-carboxamide
KY-05009