TNIK-IN-3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TNIK-IN-3 (化合物 21k) 是一种有效，选择性和具有口服活性的 TNIK 抑制剂，IC50 值为 0.026 μM。TNIK-IN-3 还可以抑制 Flt4 (IC50=0.030 μM)，Flt1 (IC50=0.191 μM) 和 DRAK1 (IC50=0.411 μM)。TNIK-IN-3 可用于结直肠癌的研究。

TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer.

TNIK-IN-3 (compound 21k) inhibits Aurora-A, GCK, and MLK3 with IC50s of 0.517 μM, 3.657 μM, and 4.552 μM, respectively.TNIK-IN-3 (0.1-100 μM; 3 days) inhibits the viability of HCT116 and DLD-1 cells, with IC50s of 4.26 μM and 8.00 μM, respectively. TNIK-IN-3 (2.5-40 μM; 10 days) dose-dependently inhibits the colony formation of HCT116 and DLD-1 cells.TNIK-IN-3 (5-20 μM; 48 h) inhibits the migration of HCT116 and DLD-1 cells.TNIK-IN-3 (5-40 μM; 48 h) dose-dependently inhibits the expression ofLRP5 and LRP6 proteins, Wnt target genes AXIN2 and c-Myc in HCT116 cells.TNIK-IN-3 (5-20 μM; 48 h) significantly suppresses the phosphorylation of JNK1/2 in Hela cells.Cell Viability Assay Cell Line:HCT116 and DLD-1 cells Concentration: 0.1-100 μM Incubation Time:3 days Result:Inhibited cell viability in a dose-dependent manner.Cell Viability Assay Cell Line:HCT116 cells Concentration:5, 10, 20, 40 μM Incubation Time:48 hours Result:Inhibited the expression of Wnt target genes AXIN2 and c-Myc, LRP5 and LRP6 proteins.

TNIK-IN-3 (compound 21k) (100-150 mg/kg; p.o. twice daily for 18 days) inhibits tumor growth in a dose-dependent manner.Animal Model:Six-week-old female NOD-SCID mice were injected with HCT116 cells Dosage:100, 150 mg/kg Administration:P.o. twice daily for 18 days Result:Significantly inhibited tumor growth at a dose of 150 mg/kg.

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Wnt/Notch/Hedgehog

Wnt/beta/catenin

Wnt/beta-catenin

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2754265-25-1

387.41

C23H18FN3O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (215.10 mM; 超声助溶 )

Fc1ccc(CN2CCOc3cc(ccc3C2=O)-c2cnc3[nH]ccc3c2)cc1

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(-20℃)

With Ice Pack

≥ 2 years