GN44028 is potent and selective HIF-1α inhibitor with IC50 ~14 nM. It inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization in nuclei under the hypoxic conditions. This suggests that GN44028 probably affected the transcriptional pathway induced by the HIF-1α/HIF-1β heterodimer.
CAS Number: 1421448-26-1
Molecular Weight: 305.33
Chemical Name: N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM; EtOH up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
GN44028 was used at 1-10 µM in vitro and cellular assays.
- Minegishi H, et al. Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors. (2013) ACS Med Chem Lett. 4(2):297-301.
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