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。
| 生物活性 | TNIK-IN-3 is a potent, selective and orally active inhibitor ofTraf2- and Nck-interacting protein kinase (TNIK), with anIC50of 0.026 μM. TNIK-IN-3 could also inhibitFlt4(IC50=0.030 μM),Flt1(IC50=0.191 μM) andDRAK1(IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectalcancer[1]. |
| IC50& Target | IC50: 0.026 μM (TNIK)[1], 0.030 μM (Flt4)[1], 0.191 μM (Flt1)[1], 0.411 μM (DRAK1)[1] |
体外研究
(In Vitro) | 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[1].
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[1].
TNIK-IN-3 (2.5-40 μM; 10 days) dose-dependently inhibits the colony formation of HCT116 and DLD-1 cells[1].
TNIK-IN-3 (5-20 μM; 48 h) inhibits the migration of HCT116 and DLD-1 cells[1].
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[1].
TNIK-IN-3 (5-20 μM; 48 h) significantly suppresses the phosphorylation of JNK1/2 in Hela cells[1].
Cell Viability Assay[1] | 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[1] | 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. |
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体内研究
(In Vivo) | TNIK-IN-3 (compound 21k) (100-150 mg/kg; p.o. twice daily for 18 days) inhibits tumor growth in a dose-dependent manner[1].
| Animal Model: | Six-week-old female NOD-SCID mice were injected with HCT116 cells[1] | | 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.
No obvious weight loss and no other side effects were observed. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(215.10 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5812 mL | 12.9062 mL | 25.8124 mL | | 5 mM | 0.5162 mL | 2.5812 mL | 5.1625 mL | | 10 mM | 0.2581 mL | 1.2906 mL | 2.5812 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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