Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HIF-1/2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α. Its inhibitory effect on HIF-2α activity is significant, with an IC 50 value of 0.92 μM. Furthermore, HIF-1/2α-IN-1 has the ability to decrease HIF-1α levels. This compound is particularly valuable for research on clear cell renal cell carcinoma (ccRCC) [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 1,520.00 | |
50 mg | 10-14 weeks | $ 1,980.00 | |
100 mg | 10-14 weeks | $ 2,500.00 |
Description | HIF-1/2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α. Its inhibitory effect on HIF-2α activity is significant, with an IC 50 value of 0.92 μM. Furthermore, HIF-1/2α-IN-1 has the ability to decrease HIF-1α levels. This compound is particularly valuable for research on clear cell renal cell carcinoma (ccRCC) [1]. |
In vitro | HIF-1/2α-IN-1 (compound #25), across a concentration range of 0.01-100 µM, effectively inhibits HIF-2α with an IC50 of 0.92 µM. At concentrations between 0-10 µM over 24 hours, it reduces HIF-2α levels by inhibiting IRE-dependent translation and also targets HIF-1α at elevated concentrations through the suppression of iron sulfur cluster assembly 2 (ISCA2) function. Furthermore, at 1 µM for 24 hours, it specifically targets ISCA2, triggering an iron starvation response. This compound additionally shows a significant reduction in cell viability in 786-0 and RCC4 cell lines, with IC50 values of 1.7 µM and 4.8 µM, respectively, and altered viability at higher levels in VHL versions of these cells. Experimental findings include diminished cell viability, decreased HIF-2α activity and protein levels, and lower HIF-1α levels without promoting proteasomal degradation, alongside a dose-dependent upregulation of IRP2 and TFRC and a decrease in FTH. RT-PCR results reveal a dose-dependent reduction in the transcription of HIF-2α target genes VEGFA and POU5F1 without impacting HIF-2α transcription. |
In vivo | HIF-1/2α-IN-1 (compound #25) administered orally at doses of 30 and 60 mg/kg daily significantly inhibited clear cell renal cell carcinoma (ccRCC) xenograft growth in NRG or Balb/c mice (6-8 weeks old, male, 10 per group), demonstrating good tolerance without notable weight loss in the subjects. |
Molecular Weight | 368.35 |
Formula | C17H16N6O4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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HIF-1/2α-IN-1 inhibitor inhibit