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TNIK-IN-3
CAS No. 2754265-25-1
TNIK-IN-3( —— )
Catalog No. M37634 CAS No. 2754265-25-1
TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 164 | In Stock |
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| 5MG | 258 | In Stock |
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| 10MG | 407 | In Stock |
|
| 25MG | 632 | In Stock |
|
| 50MG | 908 | In Stock |
|
| 100MG | 1377 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameTNIK-IN-3
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NoteResearch use only, not for human use.
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Brief DescriptionTNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM.
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DescriptionTNIK-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.
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In VitroTNIK-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.
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In VivoTNIK-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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Synonyms——
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PathwayWnt/Notch/Hedgehog
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TargetWnt/beta/catenin
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RecptorWnt/beta-catenin
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Research Area——
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Indication——
Chemical Information
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CAS Number2754265-25-1
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Formula Weight387.41
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Molecular FormulaC23H18FN3O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 83.33 mg/mL (215.10 mM; Ultrasonic )
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SMILESFc1ccc(CN2CCOc3cc(ccc3C2=O)-c2cnc3[nH]ccc3c2)cc1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Li Y, et, al. Discovery of 3,4-Dihydrobenzo[ f][1,4]oxazepin-5(2 H)-one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer Effects. J Med Chem. 2022 Jan 5.?
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