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GY1-22

Chemical Structure : GY1-22

CAS No.: 326903-84-8

GY1-22

Catalog No.: PC-49512Not For Human Use, Lab Use Only.

GY1-22 is a small molecule inhibitor against DNAJA1-mutP53R175H interacting pocket, reduces mutp53 protein expression in colon cancer cell line with p53R175H mutation.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GY1-22 is a small molecule inhibitor against DNAJA1-mutP53R175H interacting pocket, reduces mutp53 protein expression in colon cancer cell line with p53R175H mutation.
GY1-22 specifically disrupts the binding between mutp53 and DNAJA1, with no effect on antaxin-3, another protein that has been reported to bind to DNAJA1.
GY1-22 exhibited a dose-dependent effect on inhibition of mutp53 and cyclin D1 expression but induction of wtp53-activated Waf1p21 expression in P03 cells (derived from mice carrying both wtp53 and mutp53 R172H, equivalent to human mutp53R175H), inhibited cell growth with IC50 of 28 uM.
GY1-22 (1 mg/kg, i.p. injection) showed a significant inhibition of in vivo tumor growth in P03 subcutaneous implanted in C57BL/6J mice.

Physicochemical Properties

M.Wt 400.50
Formula C23H20N4OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2- {2-[(1H benzimidazol-2-ylmethyl)sulfanyl]-1H-benzimidazol-1-yl}ethyl phenyl ether

References

1. Tong X, et al. J Biol Chem. 2021 Jan-Jun;296:100098.

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