326903-84-8
326903-84-8 structure
- Name: GY1-22
- Chemical Name: GY1-22
- CAS Number: 326903-84-8
- Molecular Formula: C23H20N4OS
- Molecular Weight: 400.50
- Catalog: Signaling Pathways Apoptosis MDM-2/p53
- Create Date: 2023-05-04 15:24:58
- Modify Date: 2024-01-19 18:36:14
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GY1-22 is an inhibitor of DNAJA1-mutP53R175H interacting pocket. GY1-22 can be used for the research of cancer[1].
| Name | GY1-22 |
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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]. |
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| Related Catalog | |
| Target |
DNAJA1-mutP53R175H interacting pocket[1] |
| In Vitro | 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: 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 | 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: 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. |
| References |
| Molecular Formula | C23H20N4OS |
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| Molecular Weight | 400.50 |