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LY5

Names

[ CAS No. ]:
1436382-03-4

[ Name ]:
LY5

[Synonym ]:
1-Naphthalenesulfonamide, 5,8-dihydro-5,8-dioxo-6-(3-pyridinylamino)-
5,8-Dioxo-6-(3-pyridinylamino)-5,8-dihydro-1-naphthalenesulfonamide

Biological Activity

[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.  

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
635.6±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H11N3O4S

[ Molecular Weight ]:
329.331

[ Flash Point ]:
338.2±34.3 °C

[ Exact Mass ]:
329.047028

[ LogP ]:
0.03

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.717

Related Compounds