产品
编 号：F747429
分子式：C26H22N2O2
分子量：394.47
分子式：C26H22N2O2
分子量：394.47
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CAS No: 1826116-38-4
产品详情
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.
体内研究：
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。Animal Model:Female Swiss nude mice injected with HuH-7 cells
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.
体外研究：
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)。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。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。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。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。LMP53-2 (1.5 μM) 使 HuH-7 细胞对 Sorafenib 敏感。
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.
体内研究：
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。Animal Model:Female Swiss nude mice injected with HuH-7 cells
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.
体外研究：
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)。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。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。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。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。LMP53-2 (1.5 μM) 使 HuH-7 细胞对 Sorafenib 敏感。
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