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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 326903-84-8
分子式: C₂₃H₂₀N₄OS
分子量:400.50

保管条件:

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

Data Sheet (276 KB)

GY1-22 構造式

CAS 番号: 326903-84-8

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

体外実験

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).

体内実験

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.

化学情報

CAS 番号 326903-84-8
分子量 400.50
分子式 C₂₃H₂₀N₄OS
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (276 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

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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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