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Cat. No. Product Name CAS No. Information
PC-62044

KHS-101

1262770-73-9

KHS-101 (KHS101) is a small molecule that selectively induces a neuronal differentiation phenotype, induces neuronal differentiation in cultured hippocampal neural progenitor cells (NPCs) by interacting with TACC3 (EC50=1 uM); works indirectly on HIF complex formation by destabilizing both TACC3 and the HIF component HIF-1α, decreases TACC3 levels in cells and regulates HIF gene expression; significantly increases neuronal differentiation in rats in vivo.

PC-61213

JNJ-42905343

1238689-36-5

JNJ-42905343 is a potent, selective, orally active prolyl hydroxylase (PHD) inhibitor with pKi of 8.07, 7.48 and 7.27 for PHD1, PHD2 and PHD3 respectively; stabilizes HIF1-α in a concentration-dependent fashion in HeLa cells (EC50=19.7 uM) and stimulates the release of EPO from Hep3B cells (EC50=20.3 uM); increases blood haemoglobin, mean corpuscular haemoglobin (MCH) and mean corpuscular volume (MCV), corrects functional iron deficiency and inflammation-induced anaemia in rats.

PC-60509

Desidustat

1616690-16-4

A novel HIF prolyl hydroxylase (PHD) inhibitor under clinical development for the treatment of anemia; increases circulating EPO levels after acute treatment in mice (10.3±3.7 and 40.0±8.5 fold rise at 15 and 30 mg/kg, respectively); demonstrates hematinic potential by combined effects on EPO release and efficient iron utilization in nephrectomized rats.

PC-60370

IDF-11774

1429054-28-3

IDF-11774 (IDF 11774, IDF11774) is a potent, orally bioavailable HIF-1 inhibitor that reduces the HRE-luciferase activity of HIF-1α (IC50=3.65 uM) and blocks HIF-1α accumulation under hypoxia in HCT116 human colon cancer cells; suppresses the mRNA expression of HIF-1 target genes VEGF and EPO but not HIF-1α; inhibits the accumulation of HIF-1α in vitro and in vivo in colorectal carcinoma HCT116 cells; exhibits substantial anticancer efficacy in mouse models containing KRAS, PTEN, or VHL mutations.

PC-60317

PT-2399

1672662-14-4

PT-2399 (PT 2399, PT2399) is a selective, potent HIF-2α antagonist that binds directly to the HIF2α PAS B domain; minimally affects a panel of 68 receptors, ion channels, and enzymes; specifically disassembles HIF-2 but not HIF-1 complexes, reduces the expression of HIF-2 target genes (VEGF, SERPINE1, IGFBP3, CCND1, TGFA, and SLC2A1), but not HIF-1 targets (CA9, PGK1, and LDHA); exhibits tumor growth inhibition in selected VHL-deficient clear-cell renal cell carcinoma (ccRCC) models.

PC-45660

THS-044

62054-67-5

THS-044 is a low micromolar HIF2α PAS-B binding compound (Kd=2 uM); modulates the affinity of the HIF2α:ARNT PAS-B heterodimer in vitro.

PC-45555

KC7F2

927822-86-4

A small molecule HIF-1α translation inhibitor with IC50 of 20 uM; prevents the activation of HIF-target genes such as CA IX, MMP2, Endothelin 1, and Enolase 1; down regulates of HIF-1α protein synthesis by suppression of the phosphorylation of 4EBP1 and p70S6K.

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