TNIK-IN-3

TNIK-IN-3

T650211-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK) , with an IC 50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 ( IC 50 =0.030 μM), Flt1 ( IC 50 =0.191 μM) and DRAK1 ( IC 50 =0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer In Vitro TNIK-IN-3 (compound 21k) inhibits Aurora-A, GCK, and MLK3 with IC 50 s 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 IC 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AssayCell 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. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. No obvious weight loss and no other side effects were observed. Form:Solid IC50& Target:IC50: 0.026 μM (TNIK), 0.030 μM (Flt4), 0.191 μM (Flt1), 0.411 μM (DRAK1)

TNIK-IN-3 是一种强效、选择性和口服活性的 Traf2- 和 Nck 交互蛋白激酶（TNIK）抑制剂，其 IC 50 为 0.026 μM。TNIK-IN-3 还能抑制 Flt4（IC 50 =0.030 μM）、Flt1（IC 50 =0.191 μM）和 DRAK1（IC 50 =0.411 μM）。TNIK-

2754265-25-1

C23H18FN3O2

387.41 g/mol

O=C1C2=CC=C(C=C2OCCN1CC3=CC=C(C=C3)F)C4=CC5=C(NC=C5)N=C4

DMSO : 83.33 mg/mL (215.10 mM; Need ultrasonic)