| Bioactivity | GY1-22 is an inhibitor of DNAJA1-mutP53R175H interacting pocket. GY1-22 can be used for the research of cancer[1]. |
| Target | DNAJA1-mutP53R175H interacting pocket |
| Invitro | GY1-22 (0-50 μM; 24 h) 降低小鼠胰腺癌 P03 和人结肠癌 LS123 细胞中突变 p53 蛋白的表达。GY1-22 在 mutp53 驱动的 P03 细胞中抑制 cyclin D1 表达并诱导 wtp53 激活的 Waf1p21 表达[1]。在 DNAJA1-mutp53 R175H 复合物界面的关键位点发生突变后，GY1-22 失去了降解 mutp53R175H 的能力[1]。GY1-22 (0-100 μM; 24 h) 在 mutp53 驱动的 P03 胰腺癌细胞中剂量依赖性地抑制细胞生长和显示出低细胞毒性[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | GY1-22 在大鼠中的 LD50 为 1240 mg/kg。剂量为 10mg /kg (i.p.; daily for 2 weeks) 时对小鼠在大体上或组织学上没有表现出任何毒性[1]。GY1-22 (1 mg/kg; i.p.; daily for 2 weeks) 在小鼠中抑制 mutp53 驱动的 P03 胰腺癌细胞生长[1]。 Animal Model: |
| Name | GY1-22 |
| CAS | 326903-84-8 |
| Formula | C23H20N4OS |
| Molar Mass | 400.50 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |