Name | (4-methoxyphenyl)-morpholin-4-yl-sulfanylidene-sulfido-λ5-phosphane,morpholin-4-ium |
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Synonyms |
Phosphinodithioic acid, P-(4-methoxyphenyl)-P-4-morpholinyl-, compd. with morpholine (1:1)
gyy 4137 (4-Methoxyphenyl)4-morpholinylphosphinodithioic acid - morpholine (1:1) GYY 4137 morpholine salt (4-Methoxyphenyl)morpholino-phosphinodithioic acid compound with morpholine |
Description | GYY4137 is a slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity[1][2][3]. |
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Related Catalog | |
In Vitro | GYY4137 (400-800 µM) causes concentration-dependent killing of seven different human cancer cell lines (HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS) but did not affect survival of normal human lung fibroblasts (IMR90, WI-38)[2]. GYY4137 (0.1-0.5 mM) decreases LPS-induced production of nitrite (NO2−), PGE2, TNF-α and IL-6 from human synoviocytes (HFLS) and articular chondrocytes (HAC), reduces the levels and catalytic activity of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and reduced LPS-induced NF-κB activation[3]. Cell Viability Assay[2] Cell Line: HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS Concentration: 400 or 800 µM Incubation Time: 5 days Result: Significantly affected cancer cell survivability. |
In Vivo | GYY4137 (100-300 mg/kg; i.p.; daily for 14 days) significantly reduces the tumor volume in both animal models, in a dose-dependent manner[2]. In the complete Freund's adjuvant (CFA)-treated mouse, GYY4137 (50 mg/kg, i.p.) injected 1 hr prior to CFA increased knee joint swelling while an anti-inflammatory effect, as demonstrated by reduced synovial fluid myeloperoxidase (MPO) and N-acetyl-β-D-glucosaminidase (NAG) activity and decreased TNF-α, IL-1β, IL-6 and IL-8 concentration, was apparent when GYY4137 was injected 6 hrs after CFA[3]. GYY4137 significantly inhibited tumor growth in the subcutaneous HepG2 xenograft model by inhibiting STAT3 activation and its target gene expression[4]. GYY4137 prevents nitrative stress and α-synuclein nitration in an MPTP mouse model of parkinson’s disease[5]. Animal Model: Female, severe combined immunodeficiency (SCID) mice (bearing HL-60 or MV4-11 cells) [2] Dosage: 100, 200 and 300 mg/kg Administration: I.p.; daily for 14 days Result: Reduced tumor volume by 52.5±9.2% and 55.3±5.7% in HL-60 and MV4–11 injected animals. |
References |
Melting Point | 164-166 ºC |
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Molecular Formula | C15H25N2O3PS2 |
Molecular Weight | 376.474 |
Exact Mass | 376.104431 |
PSA | 89.44000 |
LogP | 2.24680 |
~67% 106740-09-4 |
Literature: PENINSULA COLLEGE OF MEDICINE AND DENTISTRY, UNIVERSITY OF EXETER; WHITEMAN, Matthew; HANCOCK, John; WILSON, Ian; LISJAK, Miroslav Patent: WO2012/42227 A1, 2012 ; Location in patent: Page/Page column 21 ; |
Precursor 2 | |
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DownStream 0 |