(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物
(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物
(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物 性质
| 熔点 | 164-166℃ |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | DMF:20mg/mL; DMSO:15mg/mL; PBS(pH 7.2):3 mg/mL |
| 形态 | 白色固体。 |
| 颜色 | 白色 |
| 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 |
| InChIKey | YZMHNNLDUWRZFW-UHFFFAOYSA-N |
| SMILES | C1C(OC)=CC=C(P([S-])(N2CCOCC2)=S)C=1.C1C[N+]([H])([H])CCO1 |
(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物 用途与合成方法
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.
Cell Viability Assay
| Cell Line: | HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS |
| Concentration: | 400 or 800 µM |
| Incubation Time: | 5 days |
| Result: | Significantly affected cancer cell survivability. |
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.
| Animal Model: | Female, severe combined immunodeficiency (SCID) mice (bearing HL-60 or MV4-11 cells) |
| Dosage: | 100, 200 and 300 mg/kg |
| Administration: | I.p.; daily for 14 days |
| Result: | Reduced tumor volume by 52.5±9.2% and 55.3±5.7% in HL-60 and MV4–11 injected animals. |
(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-09-15 | HY-107632 | (4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物 | 106740-09-4 | 5 mg | 350 |
| 2026-09-15 | HY-107632 | (4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物 | 106740-09-4 | 10mg | 550 |