GYY4137

GYY4137 is a slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity.

Product information

CAS Number: 106740-09-4

Molecular Weight: 376.47

Formula: C15H25N2O3PS2

Chemical Name: (4-methoxyphenyl)(morpholin-4-yl)sulfanyl-λ⁵-phosphanethione; morpholine

Smiles: COC1C=CC(=CC=1)P(S)(=S)N1CCOCC1.C1COCCN1

InChiKey: YZMHNNLDUWRZFW-UHFFFAOYSA-N

InChi: InChI=1S/C11H16NO2PS2.C4H9NO/c1-13-10-2-4-11(5-3-10)15(16,17)12-6-8-14-9-7-12;1-3-6-4-2-5-1/h2-5H,6-9H2,1H3,(H,16,17);5H,1-4H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (265.63 mM; Need ultrasonic). H2O : 19.23 mg/mL (51.08 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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 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.

Products are for research use only. Not for human use.