| Identification | Back Directory | [Name]
(3S,9bR)-2,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methyl]-9b-phenyloxazolo[2,3-a]isoindol-5(9bH)-one | [CAS]
1826116-38-4 | [Synonyms]
SLMP53-2
(3S,9bR)-3-[(1-Methyl-3-indolyl)methyl]-9b-phenyl-2,3-dihydrooxazolo[2,3-a]isoindol-5(9bH)-one
(3S,9bR)-2,3-Dihydro-3-[(1-methyl-1H-indol-3-yl)methyl]-9b-phenyloxazolo[2,3-a]isoindol-5(9bH)-one | [Molecular Formula]
C26H22N2O2 | [MOL File]
1826116-38-4.mol | [Molecular Weight]
394.47 |
| Chemical Properties | Back Directory | [Boiling point ]
615.4±55.0 °C(Predicted) | [density ]
1.27±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [form ]
Solid | [pka]
-2.69±0.60(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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 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]. | 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. |
| [References]
[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. DOI:10.3390/cancers11081151
[2] Loureiro JB, et, al. Mutant p53 reactivator SLMP53-2 hinders ultraviolet B radiation-induced skin carcinogenesis. Pharmacol Res. 2022 Jan;175:106026. DOI:10.1016/j.phrs.2021.106026 |
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