2. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage Apoptosis
  3. GSK-3 CDK Apoptosis
  4. GTGKT

GTGKT 是一种 CAGE 抑制剂。GTGKT 与 CAGE 结合，并阻止 CAGE 与 GSK3β 的结合。GTGKT 改变 CAGE 的定位，并抑制 CAGE 与 Cyclin D1 启动子序列的结合。GTGKT 增强抗癌剂的凋亡 (Apoptotic) 作用。GTGKT 可降低 Cyclin D1 的表达。GTGKT 降低黑色素瘤和肝细胞癌细胞的致瘤潜能。


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Custom Peptide Synthesis

GTGKT

GTGKT Chemical Structure

CAS No. : 254732-11-1

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GTGKT 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GTGKT is a CAGE inhibitor. GTGKT binds to CAGE and blocks the binding of CAGE to GSK3β. GTGKT alters the localization of CAGE and inhibits the binding of CAGE to the promoter sequence of Cyclin D1. GTGKT enhances the Apoptotic effect of anticancer agents. GTGKT reduces the expression of Cyclin D1. GTGKT decreases the tumorigenic potential of melanoma and hepatocellular carcinoma cells[1].

IC50 & Target[1]

GSK-3β

 

体外研究
(In Vitro)

GTGKT (10 μM; 48 h) 在 Malme3MR-Taxol 癌细胞中可降低 cyclinD1 和 pGSK3βSer9 的表达，抑制 CAGE-GSK3β 的结合[1]。
GTGKT (10 μM; 48 h) 可降低抗癌剂耐受的 Malme3MR 黑色素瘤细胞的迁移和侵袭能力[1]。

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

GTGKT 相关抗体:

Western Blot Analysis[1]

Cell Line: anti-cancer agent-resistant Malme3MR, SNU387R, and Malme3MR-Taxol cancer cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Decreased the expression of cyclinD1 and inactive pGSK3βSer9 without altering CAGE expression in Malme3MR, SNU387R, and Malme3MR-Taxol cells.
Inhibited the binding of CAGE to GSK3β in all three cell lines.
Directly bound to CAGE (but not GSK3β) in Malme3MR and Malme3MR-Taxol cells for biotin-labeled peptide.
体内研究
(In Vivo)

GTGKT (每只小鼠 10-50 μg；静脉注射；5 次；35 天) 可通过下调 cyclinD1、pGSK3βSer9 和 MDR1 的表达、上调磷酸化 cyclinD1Thr286 的表达，以及抑制 CAGE-GSK3β 的结合，以剂量依赖方式减小无胸腺裸鼠的皮下黑色素瘤肿瘤体积[1]。
GTGKT (每只小鼠 10-50 μg；静脉注射；给药 5 次；持续 35 天) 可通过下调 cyclinD1、pGSK3βSer9 及 MDR1 的表达、上调磷酸化 cyclinD1Thr286 的表达并抑制 CAGE-GSK3β 的结合，在无胸腺裸鼠中呈剂量依赖性地减小皮下肝细胞癌的肿瘤体积[1]。

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

Animal Model: BALB/c nu/nu (5-6-week-old females)[1]
Dosage: 10 μg/mouse; 50 μg/mouse
Administration: i.v.; five times; 35 days
Result: Significantly reduced tumor volume compared to PBS control at 10 μg/mouse.
Resulted in a greater, statistically significant reduction in tumor volume compared to PBS control at 50 μg/mouse.
Decreased expression of cyclinD1, pGSK3βSer9, and MDR1 in tumor lysates.
Increased expression of phospho-cyclinD1Thr286 in tumor lysates.
Inhibited the binding of CAGE to GSK3β in tumor tissue.
Animal Model: BALB/c nu/nu (5-6-week-old females)[1]
Dosage: 10 μg/mouse; 50 μg/mouse
Administration: i.v.; five times; 35 days
Result: Significantly reduced tumor volume compared to PBS control at 10 μg/mouse.
Significantly reduced tumor volume compared to PBS control at 50 μg/mouse, with greater efficacy than the lower dose.
Decreased expression of cyclinD1, pGSK3βSer9, and MDR1 in tumor lysates.
Increased expression of phospho-cyclinD1Thr286 in tumor lysates.
Inhibited the binding of CAGE to GSK3β in tumor tissue.
Animal Model: BALB/c nu/nu (4-week-old females)[1]
Dosage: 50 μg/mouse
Administration: i.v.; five times; 4 weeks
Result: Drastically reduced the number of surface metastatic lung nodules compared to mock and GTGRT peptide controls.
Decreased expression of cyclinD1, pGSK3βSer9, and MDR1 in lung/tumor lysates.
Inhibited the binding of CAGE to GSK3β.
Animal Model: BALB/c nu/nu (5-6-week-old females)[1]
Dosage: 50 μg/mouse
Administration: i.v.; single dose
Result: Detected strong, specific fluorescence in subcutaneous Malme3MR tumors 12 hours after injection.
Observed minimal fluorescence in normal organs (kidney, liver, spleen, lung) 12 hours after injection.
分子量

462.50

Formula

C18H34N6O8
CAS 号
Sequence

Gly-Thr-Gly-Lys-Thr
Sequence Shortening

GTGKT
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

GTGKT 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

GTGKT254732-11-1GSK-3CDKApoptosisGlycogen synthase kinase-3Glycogen synthase kinase 3Cyclin dependent kinaseanti-cancer drug-resistant cancercyclin D1GSK3βathymic nude miceSNU387RMalme3MR melanoma cellsCAGEcyclin D1 promoter sequencesapoptosisHUVECInhibitorinhibitorinhibit

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