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

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.

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SLMP53-2 Chemical Structure

SLMP53-2 Chemical Structure

CAS No. : 1826116-38-4

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Description

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].

In Vitro

SLMP53-2 (3.12-50 μM; 48 h) inhibits the growth of HuH-7 and HCC1419 cells with similar IC50 values. SLMP53-2 shows significantly lower growth inhibitory activity against non-tumoral HFF-1 cells (IC50 of 50 µM)[1].
SLMP53-2 (14-28 μM; 48-72 h) induces G0/G1-phase cell cycle arrest and apoptosis in HuH-7 cells[1].
SLMP53-2 (0.9-14 μM; 14 days) displays a concentration-dependent growth inhibitory effect on colony formation in HuH-7 cells[1].
SLMP53-2 (28 μM; 24 h) increases the levels of XBP1 nuclear protein, spliced XBP1 (sXBP1) mRNA, and phosphorylated eIF2α in HuH-7 cells[1].
SLMP53-2 (14 μM; 16-48 h) increases the protein levels of MDM2, p21, GADD45, BAX, and KILLER, while downregulating survivin and VEGF, in HuH-7 cells, an effect abolished in HuH-7 p53KO cells[1].
LMP53-2 (1.5 μM) sensitizes HuH-7 cells to Sorafenib[1].

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

In Vivo

SLMP53-2 (50 mg/kg; i.p. for five administrations) reduces the tumor volume and weight in nude mice carrying HuH-7 xenografts with no apparent toxic side effects[1].

MedChemExpress (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.
Molecular Weight

394.47

Formula

C26H22N2O2

CAS No.
SMILES

O=C1C2=CC=CC=C2[C@](OC3)(C4=CC=CC=C4)N1[C@H]3CC5=CN(C)C6=CC=CC=C56

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    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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SLMP53-2
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HY-153202
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