Chemical Structure : PG3-Oc
货号: PC-23284Not For Human Use, Lab Use Only.
PG3-Oc is a small-molecule that restores p53 pathway-signaling in tumor cells with mutant-p53, activates ATF4 and upregulates p53 target genes, inhibits cell viabiltiy of p53 mutation R273H (HT29 cell) with IC50 of 31 nM.
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PG3-Oc is a small-molecule that restores p53 pathway-signaling in tumor cells with mutant-p53, activates ATF4 and upregulates p53 target genes, inhibits cell viabiltiy of p53 mutation R273H (HT29 cell) with IC50 of 31 nM.
PG3-Oc inhibits cell proliferation and induces apoptosis in mutant p53-expressing cancer cell lines with IC50 values within the nano-molar range.
PG3-Oc has a 4- to 9-fold therapeutic index in colorectal cancer cell lines as compared to normal colon cells CCD 841 Con.
PG3-Oc treatment induces caspase-8 and caspase-3 activation in CRC cell lines, and caspase activation is required for PG3-Oc-induced cell death.
PG3-Oc partially restores the p53 pathway globally.
PUMA is required for PG3-Oc-mediated cell death, induces significant downregulation of MYC and upregulation of PUMA protein levels in a panel of p53 mutant cell lines, such as HT29, DLD1, FaDu, MDA-MB-231, and MDA-MB-468. SW480 and CAL27.
PG3-Oc induces upregulation of ATF4, ATF4 is a mediator of PG3-Oc-induced p53 pathway restoration.
PG3-Oc (5 mg/kg, times weekly for 2 wk) inhibits tumor growth in the HT29 mouse xenograft model.
分子量 | 451.61 | |
分子式 | C27H37N3O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Xiaobing Tian, et al. Oncotarget. 2024 Sep 17:15:614-633.
2. Tian X, et al. Neoplasia. 2021 Mar;23(3):304-325.
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