1. Apoptosis
  2. MDM-2/p53
  3. GY1-22

GY1-22 is an inhibitor of DNAJA1-mutP53R175H interacting pocket. GY1-22 can be used for the research of cancer.

For research use only. We do not sell to patients.

GY1-22 Chemical Structure

GY1-22 Chemical Structure

CAS No. : 326903-84-8

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Description

GY1-22 is an inhibitor of DNAJA1-mutP53R175H interacting pocket. GY1-22 can be used for the research of cancer[1].

IC50 & Target

DNAJA1-mutP53R175H 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 mutp53R175H after mutation of critical sites at the interface of the DNAJA1–mutp53R175H 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.
Molecular Weight

400.50

Formula

C23H20N4OS

CAS No.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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    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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GY1-22
Cat. No.:
HY-149911
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