GYY4137

Catalog No.S9920 Batch:S992001

Technical Data

Formula	C₁₁H₁₆NO₂PS₂.C₄H₉NO
Molecular Weight	376.47	CAS No.	106740-09-4
Solubility (25°C)*	In vitro	DMSO	75 mg/mL (199.21 mM)
		Water	5 mg/mL (13.28 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

GYY4137 is a novel, water-soluble hydrogen sulfide (H2S)–releasing molecule with vasodilator and antihypertensive activity. GYY4137 shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. GYY4137 also shows anti-inflammatory activity.

Targets

STAT3 ^[2]

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 does not affect survival of normal human lung fibroblasts (IMR90, WI-38).^[4]

In vivo

In the complete Freund's adjuvant (CFA)-treated mouse, GYY4137 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, is apparent when GYY4137 was injected 6 hrs after CFA.^[3]

Protocol (from reference)

Cell Assay:^{^[4]}	Cell lines HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS Concentrations 400 µM, 800 µM Incubation Time 5 days, 8 days Method Live cell incubated with GYY4137(400 or 800 µM) are collected after 5 days and counted in triplicate after staining with trypan blue using a haemocytometer for cell viability assay. The generation of H2S from GYY4137(400 µM) is determined in aliquots (100 µl) withdrawn at timed intervals (up to 7 days) from cultured MCF-7 cells maintained in Dulbecco's modified Eagle's medium.
Animal Study:^{^[3]}	Animal Models Complete Freund Dosages 50 mg/kg Administration i.p.

Cell Assay:^{^[4]}

Cell lines
HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS
Concentrations
400 µM, 800 µM
Incubation Time
5 days, 8 days
Method
Live cell incubated with GYY4137(400 or 800 µM) are collected after 5 days and counted in triplicate after staining with trypan blue using a haemocytometer for cell viability assay. The generation of H2S from GYY4137(400 µM) is determined in aliquots (100 µl) withdrawn at timed intervals (up to 7 days) from cultured MCF-7 cells maintained in Dulbecco's modified Eagle's medium.

Animal Study:^{^[3]}

Animal Models
Complete Freund
Dosages
50 mg/kg
Administration
i.p.

References

[4] Lee ZW, et al. PLoS One. 2011;6(6):e21077.

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SHIPPING AND STORAGE
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