1. Apoptosis
  2. MDM-2/p53 Apoptosis
  3. SLMP53-2

SLMP53-2 是一种突变的 p53 再激活因子。SLMP53-2 通过增强 mutp53-Y220C 与 Hsp70 的相互作用来恢复 mutp53-Y220C 的野生型样构象和 DNA 结合能力,从而重建 p53 转录活性。 SLMP53-2 可诱导细胞周期停滞、细胞凋亡和内质网 (ER) 应激。SLMP53-2 具有抗肿瘤活性。

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SLMP53-2 Chemical Structure

SLMP53-2 Chemical Structure

CAS No. : 1826116-38-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SLMP53-2 is a mutant p53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing its interaction with the Hsp70, leading to the reestablishment of p53 transcriptional activity. SLMP53-2 can induce cell cycle arrest, apoptosis and endoplasmic reticulum (ER) stress. SLMP53-2 exhibits antitumor activity[1][2].

体外研究
(In Vitro)

SLMP53-2 (3.12-50 μM; 48 h) 抑制 HuH-7 和 HCC1419 细胞的生长,具有相似的 IC50。 SLMP53-2 对非肿瘤 HFF-1 细胞的生长抑制活性显着降低 (IC50 of 50 µM)[1]
SLMP53-2 (14-28 μM; 48-72 h) 诱导 HuH-7 细胞 G0/G1 期细胞周期停滞和细胞凋亡[1]
SLMP53-2 (0.9-14 μM; 14 days) 对 HuH-7 细胞集落形成具有浓度依赖性生长抑制作用[1]
SLMP53-2 (28 μM; 24 h) 增加 HuH-7 细胞中 XBP1 核蛋白、剪接 XBP1 (sXBP1) mRNA 和磷酸化 eIF2α 的水平[1]
SLMP53-2 (14 μM; 16-48 h) 增加 HuH-7 细胞中 MDM2、p21、GADD45、BAX 和 KILLER 的蛋白质水平,同时下调生存素和 VEGF,这种作用在 HuH-7 p53KO 细胞中被消除< sup>[1]。
LMP53-2 (1.5 μM) 使 HuH-7 细胞对 Sorafenib 敏感[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SLMP53-2 (50 mg/kg; i.p. for five administrations) 减少携带 HuH-7 异种移植物的裸鼠的肿瘤体积和重量,且无明显毒副作用[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Swiss nude mice injected with HuH-7 cells[1]
Dosage: 50 mg/kg
Administration: Twice-weekly intraperitoneal injections for five administrations
Result: Displayed anti-tumor activity in HCC xenograft mouse models.
Showed no significant variation of body weight throughout the experiment.
No significant differences were observed between the weight of spleen, liver, heart, and kidneys.
分子量

394.47

Formula

C26H22N2O2

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

SLMP53-2 相关分类

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  • 稀释计算器

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  • 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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HY-153202
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