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Belzutifan (PT2977) is a second-generation orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan (PT2977; MK-6482) inhibited clear cell renal cell carcinoma (ccRCC) potentially. Belzutifan (PT2977) potently and dose-dependently reduces mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, and leads to rapid and dose-dependent reduction in EPO expression.
| Molecular Weight | 383.34 |
| Formula | C17H12F3NO4S |
| CAS Number | 1672668-24-4 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage | -20°C, sealed |
| Related HIF Products |
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| FG-4592 (Roxadustat)
FG-4592 (Roxadustat; ASP1517) is a novel Hypoxia Inducible Factor Prolyl Hydroxylase inhibitor. |
| 2-Methoxyestradiol
2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa. |
| DMOG
DMOG (Dimethyloxaloyl glycine) is an antagonist of α-ketoglutarate cofactor and a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy. |
| IOX2
IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. |
| Hydralazine hydrochloride
Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM. |
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