MedChemExpress - Model GN44028 -1421448-26-1
GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers[1][3].MCE products for research use only. We do not sell to patients.
GN44028
MCE China：GN44028
Brand：MedChemExpress (MCE)
Cat. No.HY-110266
CAS：1421448-26-1
Purity：99.48%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.
In Vitro：GN44028 (compound 2I, 0-30 μM approximately) has anti-proliferative activities against HCT116, HepG2 and HeLa cells[1]. GN44028 (0.001-1 μM, 4 h) inhibits the hypoxia-induced VEGF mRNA expression in HeLa cells[1]. GN44028 (20 nM, 10 days) abrogates the TGF‐β‐induced colony formation in HCT116 cells[2].
In Vivo：GN44028 (10 mg/kg, oral gavage) extends the survival rate of animals in mice bearing a mixed orthotopic tumor with PN12 and ME23 cells[3]. GN44028 (5 mg/kg, tail vein injection, twice a week) suppresses tumor growth in a subcutaneous colorectal cancer model[2].
IC50 & Target：IC50: 14 nM (HIF-1α)[1]. Cellular Effect Cell Line Type Value Description References
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References：
[1]. Minegishi H, et al. Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors. ACS Med Chem Lett. 2013 Jan 27;4(2):297-301. [Content Brief]
[2]. Changfu Liu, et al. Tumor-associated macrophage-derived transforming growth factor-β promotes colorectal cancer progression through HIF1-TRIB3 signaling. Cancer Sci. 2021 Oct;112(10):4198-4207. [Content Brief]
[3]. Xiaoqing Fan, et al. Heterogeneity of subsets in glioblastoma mediated by Smad3 palmitoylation. Oncogenesis. 2021 Oct 27;10(10):72. [Content Brief]
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