2. Apoptosis Stem Cell/Wnt JAK/STAT Signaling NF-κB Immunology/Inflammation
  3. Apoptosis STAT NF-κB TNF Receptor NO Synthase Interleukin Related COX
  4. GYY4137

GYY4137 (GMP) 是 GMP 级别的 GYY4137 (HY-107632)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。GYY4137 (GMP) 是一种缓释 H2S 供体，具有血管扩张、抗高血压活性和抗炎活性。 GYY4137 (GMP) 能通过阻断 STAT3 通路，从而抑制细胞生长、诱导了细胞凋亡 (apoptosis) 和细胞周期停滞，表现出强效的抗癌活性。

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GYY4137

GYY4137 Chemical Structure

CAS No. : 106740-09-4

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GYY4137 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3][4][5][6].

IC50 & Target[6]

Stat-3

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
368.2 μM
Compound: 1, GYY4137
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
[PMID: 26147240]
MCF7 IC50
> 500 μM
Compound: 1, GYY4137
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
[PMID: 26147240]
MDA-MB-231 IC50
239.6 μM
Compound: 1, GYY4137
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
[PMID: 26147240]
PC-3 IC50
> 200 μM
Compound: 1, GYY4137
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
[PMID: 26147240]
SK-OV-3 IC50
332 μM
Compound: 1, GYY4137
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
[PMID: 26147240]
WI-38 IC50
1977 μM
Compound: 1, GYY4137
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
[PMID: 26147240]
体外研究
(In Vitro)

GYY4137 (GMP) (400-800 μM) 会导致七种不同人类癌细胞系 (HeLa、HCT-116、Hep G2、HL-60、MCF-7、MV4-11 和 U2OS) 的浓度依赖性死亡，但不影响正常人肺成纤维细胞 (IMR90、WI-38) 的存活[2]。
GYY4137 (GMP) (0.1-0.5 mM) 可减少 LPS 诱导的人类滑膜细胞 (HFLS) 和关节软骨细胞 (HAC) 产生的亚硝酸盐 (NO2 )、PGE2、TNF-α 和 IL-6，降低诱导型一氧化氮合酶 (iNOS) 和环氧合酶-2 (COX-2) 的水平和催化活性，并降低 LPS 诱导的 NF-κB 活化[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GYY4137 相关抗体:

Cell Viability Assay[2]

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.
体内研究
(In Vivo)

GYY4137 (GMP) (100-300 mg/kg；腹腔注射；每天注射 14 天) 以剂量依赖性方式显着减小两种动物模型中的肿瘤体积[2]。
在完全弗氏佐剂 (CFA) 处理的小鼠中，在 CFA 前 1 小时注射 GYY4137 (GMP)（50 mg/kg，腹腔注射）会增加膝关节肿胀，而当在 CFA 后 6 小时注射 GYY4137 (GMP) 时，其抗炎作用明显，表现为滑液髓过氧化物酶 (MPO) 和 N-乙酰-β-D-氨基葡萄糖苷酶 (NAG) 活性降低，TNF-α、IL-1β、IL-6 和 IL-8 浓度降低[3]。
GYY4137 (GMP) 通过抑制 STAT3 显着抑制皮下 HepG2 异种移植模型中的肿瘤生长激活及其靶基因表达[4]。
GYY4137 (GMP) 可防止帕金森病 MPTP 小鼠模型中的硝化应激和 α-突触核蛋白硝化[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female, severe combined immunodeficiency (SCID) mice (bearing HL-60 or MV4-11 cells)[2]
Dosage: 100, 200 and 300 mg/kg
Administration: i.p.; daily for 14 days
Result: Reduced tumor volume by 52.5% and 55.3% in HL-60 and MV4–11 injected animals.
分子量

376.47

Formula

C15H25N2O3PS2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GYY4137 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GYY4137 (GMP)106740-09-4ApoptosisSTATNF-κBTNF ReceptorNO SynthaseInterleukin RelatedCOXNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRNitric oxide synthasesNOSILCyclooxygenaseH2Sdonorvasodilatorantihypertensiveanti-inflammatoryCFAanti-hepatocellularcarcinomaparkinson’sdiseaseBel7402LO2BALB/c-nu/nu miceapoptosisInhibitorinhibitorinhibit

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