PeptideDB

SLMP53-2

CAS: 1826116-38-4 F: C26H22N2O2 W: 394.47

SLMP53-2 is a mutant p53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y2
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Bioactivity 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].
Invitro 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[1]。LMP53-2 (1.5 μM) 使 HuH-7 细胞对 Sorafenib 敏感[1]。
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]。 Animal Model:
Name SLMP53-2
CAS 1826116-38-4
Formula C26H22N2O2
Molar Mass 394.47
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]. Gomes S, et, al. SLMP53-2 Restores Wild-Type-Like Function to Mutant p53 through Hsp70: Promising Activity in Hepatocellular Carcinoma. Cancers (Basel). 2019 Aug 10;11(8):1151. [2]. Loureiro JB, et, al. Mutant p53 reactivator SLMP53-2 hinders ultraviolet B radiation-induced skin carcinogenesis. Pharmacol Res. 2022 Jan;175:106026.