GYY4137 

GYY4137 (GMP) is the GMP-grade version of GYY4137 (HY-107632). Small molecules of GMP grade can be used as adjuvant reagents in cell therapy. GYY4137 (GMP) is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GYY4137 (GMP) can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity^{[1][2][3][4][5][6]}.

GYY4137 (GMP) (400-800 μM) 会导致七种不同人类癌细胞系 (HeLa、HCT-116、Hep G2、HL-60、MCF-7、MV4-11 和 U2OS) 的浓度依赖性死亡，但不影响正常人肺成纤维细胞 (IMR90、WI-38) 的存活^[2]。
GYY4137 (GMP) (0.1-0.5 mM) 可减少 LPS 诱导的人类滑膜细胞 (HFLS) 和关节软骨细胞 (HAC) 产生的亚硝酸盐 (NO2 )、PGE2、TNF-α 和 IL-6，降低诱导型一氧化氮合酶 (iNOS) 和环氧合酶-2 (COX-2) 的水平和催化活性，并降低 LPS 诱导的 NF-κB 活化^[3]。

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

GYY4137 (GMP) (100-300 mg/kg；腹腔注射；每天注射 14 天) 以剂量依赖性方式显着减小两种动物模型中的肿瘤体积^[2]。
在完全弗氏佐剂 (CFA) 处理的小鼠中，在 CFA 前 1 小时注射 GYY4137 (GMP)（50 mg/kg，腹腔注射）会增加膝关节肿胀，而当在 CFA 后 6 小时注射 GYY4137 (GMP) 时，其抗炎作用明显，表现为滑液髓过氧化物酶 (MPO) 和 N-乙酰-β-D-氨基葡萄糖苷酶 (NAG) 活性降低，TNF-α、IL-1β、IL-6 和 IL-8 浓度降低^[3]。
GYY4137 (GMP) 通过抑制 STAT3 显着抑制皮下 HepG2 异种移植模型中的肿瘤生长激活及其靶基因表达^[4]。
GYY4137 (GMP) 可防止帕金森病 MPTP 小鼠模型中的硝化应激和 α-突触核蛋白硝化^[5]。

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

376.47

C₁₅H₂₅N₂O₃PS₂

106740-09-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]

  [6]. Lu S, et al. GYY4137, a hydrogen sulfide (H2S) donor, shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway[J]. International journal of oncology, 2014, 44(4): 1259-1267.  [Content Brief]