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GYY4137
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GYY4137
CAS No. : 106740-09-4
MCE 站:GYY4137
产品活性:GY4137 是一种缓释 H2S 供体,具有血管扩张和抗高血压活性。GY4137 还具有抗炎和抗癌活性。
研究领域:Others
作用靶点:Others
In Vitro: GYY4137 (400-800 ?M) 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).
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.
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.
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.
GYY4137 significantly inhibited tumor growth in the subcutaneous HepG2 xenograft model by inhibiting STAT3 activation and its target gene expression.
GYY4137 prevents nitrative stress and α-synuclein nitration in an MPTP mouse model of parkinson’s disease.
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