GN44028

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GN44028 是 (HIF)-1 的缺氧诱导因子抑制剂 (IC50: 14 nM)。 GN44028 抑制缺氧诱导的 HIF-1α 转录活性。

GN44028 is a hypoxia-inducible factor inhibitor of (HIF)-1 (IC50: 14 nM). GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity. However, It can not be suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.

GN44028 (compound 2I, 0-30 μM approximately) has anti-proliferative activities against HCT116, HepG2 and HeLa cells.GN44028 (0.001-1 μM, 4 h) inhibits the hypoxia-induced VEGF mRNA expression in HeLa cells.GN44028 (20 nM, 10 days) abrogates the TGF‐β‐induced colony formation in HCT116 cells. RT-PCR Cell Line:HeLa cells Concentration:0.001, 0.01, 0.1, 1μM Incubation Time:4 h Result:Inhibited the hypoxia-induced HIF-1 transcriptional activity without affecting HIF-1α/HIF-1β heterodimerization.

GN44028 (10 mg/kg, oral gavage) extends the survival rate of animals in mice bearing a mixed orthotopic tumor with PN12 and ME23 cells.GN44028 (5 mg/kg, tail vein injection, twice a week) suppresses tumor growth in a subcutaneous colorectal cancer model. Animal Model:Mice bearing a mixed orthotopic tumor with PN12 and ME23 cells Dosage:10 mg/kg Administration:Oral gavageResult:Reduced both proneural and mesenchymal markers.Animal Model:Subcutaneous colorectal cancer model (HCT116)Dosage:5 mg/kg Administration:Tail vein injection, twice a week Result:Reduced pulmonary nodules in tumor-bearing mice, and enhanced the outcome of chemotherapy.

N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine

Angiogenesis

HIF/HIF Prolyl-hydroxylase

Human Endogenous Metabolite

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1421448-26-1

305.337

C18H15N3O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (163.76 mM)

C1c2ccccc2-c2[nH]nc(Nc3ccc4OCCOc4c3)c12

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(-20℃)

With Ice Pack

≥ 2 years