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Merck
CN

5.33298

Sigma-Aldrich

TNIK Inhibitor, KY-05009

Synonym(s):

TNIK Inhibitor, KY-05009, Traf2- and Nck-interacting Kinase Inhibitor, KY-05009, KY05009, 5-(4-Methylbenzamido)-2-(phenylamino)thiazole-4-carboxamide

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About This Item

Empirical Formula (Hill Notation):
C18H16N4O2S
CAS Number:
1228280-29-2
Molecular Weight:
352.41
MDL number:
MFCD29059915
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Assay

≥98% (HPLC)

Quality Level

100

form

solid

potency

100 nM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

SMILES string

[s]1c(nc(c1NC(=O)c3ccc(cc3)C)C(=O)N)Nc2ccccc2

InChI key

WCEDGRTWDSHZHF-UHFFFAOYSA-N

Related Categories

General description

A cell-permeable, non-toxic, 2-phenylaminothiazole derivative that acts as a highly potent, ATP competitive inhibitor of Traf2- and Nck-interacting kinase (TNIK; Ki = 100 nM, IC50 = 9 nM). Also shown to inhibit the activity of MLK1 (IC50 = 18 nM). Blocks multiple effects of TGF-β1 in A549 human lung adenocarcinoma cells, including nuclear translocation of β-catenin, TNIK binding to TCF4, phosphorylation of TCF4, and phosphorylation and nuclear translocation of Smad2/3. Significantly reduces TGF-β1 induced epithelial-to-mesenchymal transition (EMT). Reduces TGF-β1-induced migration and invasion in A549 cells and inhibits gelatinase activity of MMP2 and 9. Shown to diminish TGF-β1-induced phosphorylation of focal adhesion kinase (at Tyr925), Src (at Tyr416), and paxillin (at Tyr118) and of ERK1/2 (at Thr202/Tyr204), JNK1 (Thr183/Tyr221), and JNK2 (at Thr185/Tyr223).
TNIK inhibitor, KY-05009, is a cell-permeable, highly potent inhibitor of TNIK (IC₅₀ = 9 nM). Blocks multiple effects of TGF-β1 in tumor cells.

Biochem/physiol Actions

Primary Target
TNIK

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Kim, J., et al. 2014. PLOS One.9, e110180.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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