KY-05009|cas 1228280-29-2|DC Chemicals

Cas No.:	1228280-29-2
Synonyms:	5-(4-Methylbenzamido)-2-(phenylamino)thiazole-4-carboxamide;5-[(4-Methylbenzoyl)amino]-2-(phenylamino)-4-thiazolecarboxamide
SMILES:	CC1=CC=C(C(NC2SC(NC3=CC=CC=C3)=NC=2C(=O)N)=O)C=C1
Formula:	C₁₈H₁₆N₄O₂S
M.Wt:	352.410242080688
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].
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.

Cat. No.	Product name	Field of application
DC31074	Isopropyl myristate	Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC79609	NCGC00685960	NCGC00685960 is a Nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 < 10  nM. NCGC00685960 has potent antitumor activity. NCGC00685960 increases H3K27 trimethylation levels in ovarian cancer cells and inhibits α-SMA expression in NNMT-expressing ovarian fibroblasts. NCGC00685960 reduces 1-MNA levels, reverses SAM and H3K27 hypomethylation and significantly impairs collagen contractility in cancer-associated fibroblasts (CAFs). NCGC00685960 can be used for cancers research.
DC77831	Vicadrostat	Vicadrostat (compound 29 A) is a potent and selective inhibitor of aldosterone synthase(CYP11B2) with an IC50 of 16 nM. It exhibits potential in renal disease, diabetic nephropathy, cardiovascular diseases and fibrotic disorder research.
DC77813	Zeltociclib	Zeltociclib is a cyclin-dependent kinase inhibitor with antitumor effects.
DC77714	S3226	S3226 is an inhibitor for Na+/H+ exchange subtype 3 (NHE3) with an IC50 of 0.2 µmol/L in rat NHE3 transfected fibroblasts. S3226 exhibits protective activity in rat ischemia-induced acute renal failure models.
DC77387	AUR1545	AUR1545 is a selective degrader of KAT2A and KAT2B. AUR1545 can be used in the cancer research, including studies on AML (Acute myeloid leukemia), SCLC (Small-cell carcinoma), and NEPC (Neuroendocrine Prostate Cancer).
DC77822	JNJ-77242113 (Icotrokinr)	Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.
DC77088	T025	T025 is as an orally available and potent inhibitor of Cdc2‐like kinases (CLKs) with an IC50s of 0.93 nM, 1 nM, 14 nM, 1.5 nM for CLK1, CLK2, CLK3, DYRK1B respectively. It exhibits anti‐tumor efficacy and can be used in MYC‐driven cancer research.
DC75868	AZ14133346	AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865	TI17	TI17 represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.