For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I011267 |
| CAS Number | 1421448-26-1 |
| Synonyms | N-(2,3-dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine |
| Molecular Formula | C18H15N3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C18H15N3O2/c1-2-4-13-11(3-1)9-14-17(13)20-21-18(14)19-12-5-6-15-16(10-12)23-8-7-22-15/h1-6,10H,7-9H2,(H2,19,20,21) |
| InChIKey | CGZKSZVSWAAUHE-UHFFFAOYSA-N |
| SMILES | C1COC2=C(O1)C=CC(=C2)NC3=NNC4=C3CC5=CC=CC=C54 |
| Reference | [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. [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. [3]. Xiaoqing Fan, et al. Heterogeneity of subsets in glioblastoma mediated by Smad3 palmitoylation. Oncogenesis. 2021 Oct 27;10(10):72. |
