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  3. TNIK-IN-3

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.

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TNIK-IN-3

TNIK-IN-3 構造式

CAS 番号 : 2754265-25-1

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 363 在庫あり
Solution
10 mM * 1 mL in DMSO USD 363 在庫あり
Solid
5 mg $330 在庫あり
10 mg $520 在庫あり
25 mg $830 在庫あり
50 mg $1250 在庫あり
100 mg $1850 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

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[1].

IC50 & Target

IC50: 0.026 μM (TNIK)[1], 0.030 μM (Flt4)[1], 0.191 μM (Flt1)[1], 0.411 μM (DRAK1)[1]

Cellular Effect
Cell Line Type Value Description References
DLD-1 IC50
8 3
Compound: 21k
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 34985886]
DLD-1 IC50
8 3
Compound: 21k
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 34985886]
DLD-1 IC50
8 3
Compound: 21k
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 34985886]
HCT-116 IC50
4.26 3
Compound: 21k
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 34985886]
HCT-116 IC50
4.26 3
Compound: 21k
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 34985886]
HCT-116 IC50
4.26 3
Compound: 21k
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
[PMID: 34985886]
体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
体内実験

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].

MedChemExpress (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[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.
分子量

387.41

分子式

C23H18FN3O2

CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 83.33 mg/mL (215.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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純度とドキュメンテーション

純度: 99.79%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5812 mL 12.9062 mL 25.8124 mL 64.5311 mL
5 mM 0.5162 mL 2.5812 mL 5.1625 mL 12.9062 mL
10 mM 0.2581 mL 1.2906 mL 2.5812 mL 6.4531 mL
15 mM 0.1721 mL 0.8604 mL 1.7208 mL 4.3021 mL
20 mM 0.1291 mL 0.6453 mL 1.2906 mL 3.2266 mL
25 mM 0.1032 mL 0.5162 mL 1.0325 mL 2.5812 mL
30 mM 0.0860 mL 0.4302 mL 0.8604 mL 2.1510 mL
40 mM 0.0645 mL 0.3227 mL 0.6453 mL 1.6133 mL
50 mM 0.0516 mL 0.2581 mL 0.5162 mL 1.2906 mL
60 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0755 mL
80 mM 0.0323 mL 0.1613 mL 0.3227 mL 0.8066 mL
100 mM 0.0258 mL 0.1291 mL 0.2581 mL 0.6453 mL
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
TNIK-IN-3
製品番号:
HY-145293
数量:
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