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

GY1-22 是 DNAJA1-mutP53R175H 相互作用的抑制剂。GY1-22 可用于癌症的研究。

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GY1-22 Chemical Structure

GY1-22 Chemical Structure

CAS No. : 326903-84-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]

体外研究
(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]

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).
体内研究
(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]

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.
分子量

400.50

Formula

C23H20N4OS

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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Help & FAQs
  • Do most proteins show cross-species activity?

    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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产品名称:
GY1-22
目录号:
HY-149911
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