TNIK-IN-3 - ≥99% , CAS No.2754265-25-1

CAS: 2754265-25-1 Cat. No.: T650211 Molecular Weight: 387.41

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

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)

Specifications

Specifications & Purity

≥99%

Biochemical and Physiological Mechanisms

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-

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Purity

≥99%

Names and Identifiers

• Canonical Smiles: O=C1C2=CC=C(C=C2OCCN1CC3=CC=C(C=C3)F)C4=CC5=C(NC=C5)N=C4
• Molecular Weight: 387.41

Chemical and Physical Properties

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