1172133-28-6

1172133-28-6 structure

Name: HO-3867
Chemical Name: 4-Piperidinone, 1-[(2,5-dihydro-1-hydroxy-2,2,5,5-tetramethyl-1H-pyrrol-3-yl)methyl]-3,5-bis[(4-fluorophenyl)methylene]-, (3E,5E)
CAS Number: 1172133-28-6
Molecular Formula: C₂₈H₃₀F₂N₂O₂
Molecular Weight: 464.54700
Catalog: Biochemical Inhibitor Tyrosine protein kinase/signal transducer and transcriptional activator inhibitor (JAK/STAT) STAT inhibitor
Create Date: 2016-04-30 21:56:05
Modify Date: 2024-01-08 09:50:39
HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity.

Name	4-Piperidinone, 1-[(2,5-dihydro-1-hydroxy-2,2,5,5-tetramethyl-1H-pyrrol-3-yl)methyl]-3,5-bis[(4-fluorophenyl)methylene]-, (3E,5E)
Synonyms	HO-3867

Description	HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity.
Related Catalog	Signaling Pathways >> JAK/STAT Signaling >> STAT Signaling Pathways >> Stem Cell/Wnt >> STAT Research Areas >> Cancer
Target	STAT3
In Vitro	HO-3867 exhibit minimal toxicity toward noncancerous cells and tissues but induce apoptosis in ovarian cancer cells. HO-3867 inhibit cell migration/invasion and survival by inhibiting STAT3 phosphorylation[1]. BRCA-mutated ovarian cancer cells treated with HO-3867 exhibited a significant degree of apoptosis with elevated levels of cleaved caspase-3, caspase-7 and PARP[2]. HO-3867 shows good antitumor activity at the concentration of 2 μmol/L in PANC-1 and BXPC-3 cells. Importantly, it is also found that HO-3867 treatment significantly induced reactive oxygen species (ROS) production in human pancreatic cancer cell lines, inducing PANC-1 and BXPC-3 cells[3].
References	[1]. Rath KS et al. HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer. Cancer Res. 2014 Apr 15;74(8):2316-27. [2]. Tierney BJ et al. HO-3867, a STAT3 inhibitor induces apoptosis by inactivation of STAT3 activity in BRCA1-mutated ovarian cancer cells. Cancer Biol Ther. 2012 Jul;13(9):766-75 [3]. Hu Y, et al. A novel STAT3 inhibitor HO-3867 induces cell apoptosis by reactive oxygen species-dependent endoplasmic reticulum stress in human pancreatic cancer cells. Anticancer Drugs. 2017 Apr;28(4):392-400.