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Art. -Nr.: HY-149911

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GY1-22

GY1-22 is an inhibitor of DNAJA1-mutP53^R175H interacting pocket. GY1-22 can be used for the research of cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 326903-84-8
Formel: C₂₃H₂₀N₄OS
Molecular Weight:400.50

Speicherung:

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

Data Sheet (276 KB)

GY1-22 Chemical Structure

CAS. Nr.: 326903-84-8

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GY1-22 is an inhibitor of DNAJA1-mutP53^R175H interacting pocket. GY1-22 can be used for the research of cancer^[1].

IC₅₀ & Target

DNAJA1-mutP53^R175H interacting pocket^[1]

In Vitro

GY1-22 (0-50 μM; 24 h) reduces mutp53 protein expression in mouse pancreatic cancer P03 and human colon cancer LS123 cells. GY1-22 inhibits cyclin D1 expression and induces wtp53-activated Waf1p21 expression in mutp53-driven P03 cells^[1].
GY1-22 loses the ability to degrade mutp53^R175H after mutation of critical sites at the interface of the DNAJA1–mutp53^R175H complex^[1].
GY1-22 (0-100 μM; 24 h) shows a dose-dependent effect on inhibiting cell growth and low cytotoxicity in mutp53-driven P03 pancreatic cancer cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Mouse mutp53-driven P03 pancreatic cancer cells and human colon cancer LS123 cells
Concentration:

0, 1, 10, 25 and 50 μM
Incubation Time:

24 h
Result:

Reduced mutp53 protein expression in both cells.
Exhibited a dose-dependent effect on inhibition of mutp53 and cyclin D1 expression but induction of wtp53-activated Waf1p21 expression tested in P03 cells.

Cell Viability Assay^[1]

Cell Line:

Mouse mutp53-driven P03 pancreatic cancer cells
Concentration:

0, 25, 50, 75 and 100 μM
Incubation Time:

24 h
Result:

Showed a dose-dependent effect on inhibiting cell growth with IC₅₀ of 28 μM and low cytotoxicity (cell viability).

In Vivo

The LD₅₀ of GY1-22 in rats is 1240 mg/kg. Dosage of 10 mg/kg (i.p.; daily for 2 weeks) does not exhibit any toxicity grossly or histologically in mice^[1].
GY1-22 (1 mg/kg; i.p.; daily for 2 weeks) inhibits mutp53-driven P03 pancreatic cancer cell growth in mice^[1].

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

Animal Model:

C57BL/6J mice implanted with P03 cells^[1]
Dosage:

1 mg/kg
Administration:

IP, daily for 2 weeks
Result:

Showed a significant inhibition of in vivo tumor growth, which was comparable with P03 DNAJA1 knockout line.

Chemical Information

CAS. Nr. 326903-84-8
Molecular Weight 400.50
Formel C₂₃H₂₀N₄OS
SMILES

C1(N=C(SCC2=NC3=C(N2)C=CC=C3)N4CCOC5=CC=CC=C5)=C4C=CC=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tong X, et al. Identification of a druggable protein-protein interaction site between mutant p53 and its stabilizing chaperone DNAJA1. J Biol Chem. 2021 Jan-Jun;296:100098. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

100 mg

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