1436382-03-4

1436382-03-4 structure

Name: LY5
Chemical Name: 5,8-Dioxo-6-(3-pyridinylamino)-5,8-dihydro-1-naphthalenesulfonamide
CAS Number: 1436382-03-4
Molecular Formula: C₁₅H₁₁N₃O₄S
Molecular Weight: 329.331
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2021-09-12 18:53:15
Modify Date: 2024-01-30 20:02:22
LY5 is a STAT3 inhibitor with an IC50 value of 0.5 μM. LY5 induces Apoptosis and inhibits STAT3 phosphorylation. LY5 shows antitumor activity in vivo, it can be used for the research of cancer[1].

Name	5,8-Dioxo-6-(3-pyridinylamino)-5,8-dihydro-1-naphthalenesulfonamide
Synonyms	1-Naphthalenesulfonamide, 5,8-dihydro-5,8-dioxo-6-(3-pyridinylamino)- 5,8-Dioxo-6-(3-pyridinylamino)-5,8-dihydro-1-naphthalenesulfonamide

Description	LY5 is a STAT3 inhibitor with an IC50 value of 0.5 μM. LY5 induces Apoptosis and inhibits STAT3 phosphorylation. LY5 shows antitumor activity in vivo, it can be used for the research of cancer[1].
Related Catalog	Signaling Pathways >> Stem Cell/Wnt >> STAT Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> STAT
Target	IC50: 0.5 μM (STAT3)[1]
In Vitro	LY5 shows inhibition effects to U2OS, RH30 and RD2 cancer cells with IC50 values of 0.52, 0.55 and 1.39 μM, respectively[1]. LY5 (0.25-1 μM; 16 h) induces apoptosis and inhibits STAT3 phosphorylation in human sarcoma cancer cells[1]. LY5 (0.25-1 μM; 5 h) inhibits STAT3 phosphorylation induced by IL-6[1]. Western Blot Analysis[1] Cell Line: RH30 and EW8 cell lines Concentration: 0.25-1 μM Incubation Time: 16 hours Result: Completely inhibited Tyr705 phosphorylation at 0.5 μM and dose-dependently decreased in formation of P-STAT3.
In Vivo	LY5 (5 mg/kg; i.p. once daily for 21 days) inhibits breast tumor growth in vivo[1]. Animal Model: Nude mice with MDA-MB-231 cancer cells injection[1] Dosage: 5 mg/kg Administration: Intraperitoneal injection; 5 mg/kg; once daily; for 21 days Result: Suppressed tumor growth and significantly reduced the tumor sizes.
References	[1]. Yu W, et al. Discovery of novel STAT3 small molecule inhibitors via in silico site-directed fragment-based drug design. J Med Chem. 2013 Jun 13;56(11):4402-12.