country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-P11782

Copy Link Print Information

GTGKT

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 254732-11-1
화학식: C₁₈H₃₄N₆O₈
분자량:462.50

보관:

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

맞춤형 펩타이드 합성

GTGKT Chemical Structure

CAS No.: 254732-11-1

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

GSK-3β

All GSK-3 Isoforms :

All CDK Isoforms :

In Vitro

GTGKT (10 μM; 48 h) reduces the expressions of cyclinD1 and pGSK3β^Ser9, and inhibits the binding of CAGE-GSK3β in Malme3M^R-Taxol cancer cells^[1].
GTGKT (10 μM; 48 h) reduces the migration and invasion capacities of anticancer agent-resistant Malme3M^R melanoma cells^[1].

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

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 pGSK3β^Ser9 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 Malme3M^R and Malme3M^R-Taxol cells for biotin-labeled peptide.

In Vivo

GTGKT (10-50 μg/mouse; i.v.; five times; 35 days) dose-dependently reduces subcutaneous melanoma tumor volume in athymic nude mice by decreasing cyclinD1, pGSK3β^Ser9, and MDR1 expression, increasing phospho-cyclinD1^Thr286 expression, and inhibiting CAGE-GSK3β binding^[1].
GTGKT (10-50 μg/mouse; i.v.; five times; 35 days) dose-dependently reduces subcutaneous hepatocellular carcinoma tumor volume in athymic nude mice by decreasing cyclinD1, pGSK3β^Ser9, and MDR1 expression, increasing phospho-cyclinD1^Thr286 expression, and inhibiting CAGE-GSK3β binding^[1].

MedChemExpress (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.

Chemical Information

CAS No. 254732-11-1
분자량 462.50
화학식 C₁₈H₃₄N₆O₈
Sequence

Gly-Thr-Gly-Lys-Thr
Sequence Shortening

GTGKT
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Kim Y, et al. The pentapeptide Gly-Thr-Gly-Lys-Thr confers sensitivity to anti-cancer drugs by inhibition of CAGE binding to GSK3β and decreasing the expression of cyclinD1. Oncotarget. 2017;8(8):13632-13651. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

견적 받기 해외재고보유

Other size

견적 받기

Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

GTGKT

All GSK-3 Isoforms

All CDK Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

GTGKT Related Classifications

HY-P11782 Related Classifications