| DC10436 |
SYP-5
|
SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis. |
| DC9811 |
PT2399
|
PT2399(PT=2399) is a novel HIF2α Antagonist. |
| DC11782 |
IDF-11774
|
IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM. |
| DC11607 |
JTZ-951(Enarodustat)
|
A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2. |
| DC73836 |
MO-2097
|
MO-2097 is a small molecule hnRNPA2B1-binding compound (ITC KD=43.1 uM) that suppresses hnRNPA2B1-induced HIF-1α protein expression under hypoxic and mimetic hypoxia. |
| DC73835 |
FG-0041
|
FG-0041 (FG0041) is a small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 of 2 uM for collagen prolyl hydroxylase. |
| DC73834 |
ER-400583-00
|
ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM. |
| DC72867 |
Belzutifan
|
Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay).
PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells.
PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model
In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d. |
| DC72414 |
Steppogenin
|
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors. |
| DC71830 |
Zifcasiran
|
Zifcasiran is a hypoxia-inducible factor (HIF) synthesis reducer. Zifcasiran shows antitumor activities and can be used in advanced renal cell carcinoma research. |
