GYY4137 

GYY4137 is a slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity^[1][2][3].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

376.47

Solid

C₁₅H₂₅N₂O₃PS₂

106740-09-4

SP(N1CCOCC1)(C2=CC=C(OC)C=C2)=S.N3CCOCC3

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

• [1]. Li L, et al. Characterization of a novel, water-soluble hydrogen sulfide-releasing molecule (GYY4137): new insights into the biology of hydrogen sulfide. Circulation. 2008;117(18):2351-2360.  [Content Brief]

  [2]. Lee ZW, et al. The slow-releasing hydrogen sulfide donor, GYY4137, exhibits novel anti-cancer effects in vitro and in vivo. PLoS One. 2011;6(6):e21077.  [Content Brief]

  [3]. Li L, et al. The complex effects of the slow-releasing hydrogen sulfide donor GYY4137 in a model of acute joint inflammation and in human cartilage cells. J Cell Mol Med. 2013;17(3):365-376.  [Content Brief]

  [4]. Lu S, Gao Y, et al. GYY4137, a hydrogen sulfide (H₂S) donor, shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. Int J Oncol. 2014;44(4):1259-1267.  [Content Brief]

  [5]. Hou X, et al. GYY4137, an H2S Slow-Releasing Donor, Prevents Nitrative Stress and α-Synuclein Nitration in an MPTP Mouse Model of Parkinson's Disease. Front Pharmacol. 2017;8:741. Published 2017 Oct 30.  [Content Brief]