1. Stem Cell/Wnt Apoptosis
  2. Wnt c-Myc Apoptosis
  3. TNIK-IN-10

TNIK-IN-10 (Compound N15) 是一种 TNIK 抑制剂,对人源 TNIKIC50 为 0.49 nM。TNIK-IN-10 可抑制 TNIK 的酶活性,下调 Wnt 通路靶基因 c-MycAXIN2 的表达,下调 LRP5LRP6 蛋白表达。TNIK-IN-10 诱导凋亡 (Apoptosis)。TNIK-IN-10 对结直肠癌具有抗癌活性。TNIK-IN-10 可用于结直肠癌的研究。

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TNIK-IN-10

TNIK-IN-10 Chemical Structure

CAS No. : 3112758-72-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TNIK-IN-10 (Compound N15) is a TNIK inhibitor with an IC50 of 0.49 nM against human TNIK. TNIK-IN-10 inhibits the enzymatic activity of TNIK, downregulates the expression of Wnt pathway target genes c-Myc and AXIN2, and reduces the protein expression of LRP5 and LRP6. TNIK-IN-10 induces apoptosis. TNIK-IN-10 exhibits anticancer activity against colorectal cancer. TNIK-IN-10 can be used in the research of colorectal cancer[1].

体外研究
(In Vitro)

TNIK-IN-10 (60 min) 可强效抑制重组人 TNIK 酶活性,其 IC50 为 0.49 nM[1]
TNIK-IN-10 在人肝微粒体中表现出较高的代谢稳定性,半衰期为 241 min[1]
TNIK-IN-10 (72 h) 可强效抑制结直肠癌细胞 HCT116 的增殖,其 IC50 为 2.24 ± 0.87 μM[1]
TNIK-IN-10 (1.9-7.5 μM; 72 h) 可呈剂量依赖性诱导结直肠癌细胞 HCT116 发生细胞凋亡[1]
TNIK-IN-10 (1.9-7.5 μM; 72 h) 可改变 HCT116 人结直肠癌细胞的细胞周期进程,经 72 h 处理后会降低 G1 期细胞占比并增加 S 期细胞占比[1]

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

Western Blot Analysis[1]

Cell Line: HCT116 human colorectal cancer cells
Concentration: 1.9-15 μM
Incubation Time: 48 h
Result: Reduced protein expression of Wnt target genes c-Myc and AXIN2, and downregulated LRP5 and LRP6 protein levels in a dose-dependent manner; TNIK protein expression remained unchanged.
体内研究
(In Vivo)

TNIK-IN-10 (30-50 mg/kg;腹腔注射;给 5 天/停 2 天,持续 16 天) 可在 BALB/c 裸鼠中强效且呈剂量依赖性地抑制 HCT116 异种移植瘤的生长[1]

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

Animal Model: BALB/c nude (male, 6 weeks old, 19-22 g, subcutaneous xenograft)[1]
Dosage: 30 mg/kg; 50 mg/kg
Administration: i.p.; 5-days-on/2-days-off; 16 days
Result: Achieved a tumor growth inhibition (TGI) rate of 69.6% at 50 mg/kg.
Markedly reduced tumor weights in both 30 mg/kg and 50 mg/kg treatment groups.
Induced transient body weight reductions early in treatment, which subsequently stabilized.
分子量

465.55

Formula

C28H27N5O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 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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产品名称:
TNIK-IN-10
目录号:
HY-181930
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