Chemical Structure : HIF-2α inhibitor AT-1
CAS No.:
391221-30-0
HIF-2α inhibitor AT-1
Catalog No.: PC-25845Not For Human Use, Lab Use Only.
HIF-2α inhibitor AT-1 is a small molecule hypoxia-inducible factor 2-alpha (HIF-2α) agonist with EC50 of 1.84 uM and Emax=233%, binds to HIF-2α-PAS-B domain with ITC KD of 2.63 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
HIF-2α inhibitor AT-1 is a small molecule hypoxia-inducible factor 2-alpha (HIF-2α) agonist with EC50 of 1.84 uM and Emax=233%, binds to HIF-2α-PAS-B domain with ITC KD of 2.63 uM.
AT-1 binds to HIF-2α-PAS-B with rapid association and dissociation, yielding a KD of 3.60 μM for binding kinetics and 3.20 μM for affinity in SPR assays.
AT-1 (10-40 uM) activates HIF-2α signaling in 786-O and Hep3B cells, upregulates the expression of HIF-2α target genes, including VEGFA, EPO, and SERPINE1 (PAI-1).
AT-1 significantly promotes EPO secretion in Hep3B cells.
AT-1 (10 μM or 50 μM) exhibits anemia-ameliorating potential in doxorubicin-induced zebrafish anemia mode, shows a potential synergistic effect with PHD inhibitor Molidustat.
AT-1 potentiates the therapeutic efficacy of Molidustat in adenine-induced CKD anemia mouse model.
Physicochemical Properties
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M.Wt
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336.41
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Formula
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C19H16N2O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(5-acetyl-4-phenylthiazol-2-yl)-2-methylbenzamide
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References
1. Chu SQ, et al. Acta Pharmacol Sin. 2025 Oct 1. doi: 10.1038/s41401-025-01657-w.
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