| S8886 |
Belzutifan (PT2977) |
Belzutifan (PT2977), an orally active and selective HIF-2α inhibitor, increases potency and improves pharmacokinetic profile, providing a potential treatment for clear cell renal cell carcinoma (ccRCC). |
Selective |
HIF-2α, IC50: 9 nM |
| S8352 |
PT2385 |
PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity. |
Selective |
HIF-2α, EC50: 27 nM |
| S8351 |
PT2399 |
PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. |
Pan |
|
| S1233 |
2-Methoxyestradiol (2-MeOE2) |
2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. |
Pan |
|
| S6684 |
IOX4 |
IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. IOX4 induces HIFα in various mouse tissues and human cell lines. |
Pan |
|
