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.
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- CAS. Nr.: 106740-09-4
- Formel: C15H25N2O3PS2
- Molecular Weight:376.47
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Stat-3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
>500 μM
Compound: 1, GYY4137
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Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
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[PMID: 26147240] |
| MCF7 | IC50 |
368.2 μM
Compound: 1, GYY4137
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Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
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[PMID: 26147240] |
| MDA-MB-231 | IC50 |
239.6 μM
Compound: 1, GYY4137
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Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
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[PMID: 26147240] |
| PC-3 | IC50 |
>200 μM
Compound: 1, GYY4137
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Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
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[PMID: 26147240] |
| SK-OV-3 | IC50 |
332 μM
Compound: 1, GYY4137
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Cytotoxicity against human SKOV3 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
Cytotoxicity against human SKOV3 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
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[PMID: 26147240] |
| WI-38 | IC50 |
1977 μM
Compound: 1, GYY4137
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Toxicity in human WI38 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
Toxicity in human WI38 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
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[PMID: 26147240] |
GYY4137 (GMP) (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 (GMP) (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.
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Cell Line:HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS
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Concentration:400 or 800 µM
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Incubation Time:5 days
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Result:Significantly affected cancer cell survivability.
In the complete Freund's adjuvant (CFA)-treated mouse, GYY4137 (GMP) (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 (GMP) was injected 6 hrs after CFA[3].
GYY4137 (GMP) significantly inhibited tumor growth in the subcutaneous HepG2 xenograft model by inhibiting STAT3 activation and its target gene expression[4].
GYY4137 (GMP) 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.
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Animal Model:Female, severe combined immunodeficiency (SCID) mice (bearing HL-60 or MV4-11 cells)[2]
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Dosage:100, 200 and 300 mg/kg
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Administration:i.p.; daily for 14 days
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Result:Reduced tumor volume by 52.5% and 55.3% in HL-60 and MV4–11 injected animals.
Chemical Information
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CAS. Nr. 106740-09-4
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Molecular Weight 376.47
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Formel C15H25N2O3PS2
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SMILES
SP(N1CCOCC1)(C2=CC=C(OC)C=C2)=S.N3CCOCC3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GYY4137 (GMP) Related Classifications
HY-107632G Related Classifications
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