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PG3

Chemical Structure : PG3

CAS No.: 1388227-33-5

PG3 (p53 activator, ATF4 activator PG3)

Catalog No.: PC-23283Not For Human Use, Lab Use Only.

PG3 is a small-molecule that restores p53 pathway-signaling in tumor cells with mutant-p53, activates ATF4 through ISR via kinase HRI (Heme-Regulated Inhibitor) and upregulates p53 target genes, inhibits cell viabiltiy of p53 mutation R273H (HT29 cell) with IC50 of 36 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PG3 is a small-molecule that restores p53 pathway-signaling in tumor cells with mutant-p53, activates ATF4 through ISR via kinase HRI (Heme-Regulated Inhibitor) and upregulates p53 target genes, inhibits cell viabiltiy of p53 mutation R273H (HT29 cell) with IC50 of 36 nM.
PG3 upregulates p21, PUMA, and DR5 in five cancer cell lines with various p53 mutational statuses through ATF4 (Activating Transcriptional Factor 4) and integrated stress response (ISR) independent of p53.
PG3 induces induce cell death via the HRI/ATF4/PUMA axis.

Physicochemical Properties

M.Wt 295.39
Formula C18H21N3O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-5'-((4-ethyl-3,5-dimethyl-1H-pyrrol-2-yl)methylene)-4'-methoxy-1H,5'H-2,2'-bipyrrole

References

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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