HIF

Inhibitory Selectivity

Catalog No.	Inhibitor Name	HIF	HIF1	Other
A15530	FG-2216	****	****
A15359	KC7F2	**	**
A11237	Roxadustat
A10012	2-Methoxyestradiol			Microtubule Associated
A14319	PX-478 2HCl
A12978	BAY 87-2243

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No.	Product Name	Application	Product Information
A15358	Chetomin	HIF 抑制剂	Chetomin is reported to be an antibiotic metabolite of Chaetomium spp. which contains bacteriostatic effects on Gram-positive bacteria.
A15360	ML 228	HIF activator	ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay, HIF-1?? nuclear translocation assay, and increased VEGF expression.
A15359 SALE	KC7F2	HIF 抑制剂	KC7F2 is an inhibitor of HIF-1?? protein translation, but not transcription, that suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase (S6K).
A15895	DASA-58	PKM2 Activator	DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
A12671 SALE	GSK1278863 (Daprodustat)	HIF-prolyl hydroxylase 抑制剂	GSK1278863 is a novel HIF-prolyl hydroxylase inhibitor.
A15793 SALE	JNJ-42041935	HIF-PHD 抑制剂 II	JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
A15530 SALE	FG-2216	HIF-prolyl hydroxylase 抑制剂	FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo,
A14367	Oroxylin A	-	Oroxylin A is an O-methylated flavone, It has demonstrated activity as a dopamine reuptake inhibitor and is also a negative allosteric modulator of the benzodiazepine site of the GABAA receptor. Product Citations (1) Mai Nagasaka, .et al. Anti-Tumorigenic Activity of Chrysin from Oroxylum indicum via Non-Genotoxic p53 Activation through the ATM-Chk2 Pathway, Molecules, 2018, Jun; 23(6): 1394 PMID: 29890668
A10012 SALE	2-Methoxyestradiol	Apoptotic, antiproliferative and antiangiogenic agent	2-Methoxyestradiol is an apoptotic, antiproliferative and antiangiogenic agent. Induces p53-induced apoptosis via two pathways: activation of p38 and NF-κB; and activation of JNK and AP-1 leading to Bcl-2 phosphorylation.
A14021	Echinomycin	HIF-1?? 抑制剂	Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that controls genes involved in glycolysis, angiogenesis, migration, and invasion. Echinomycin is a cell-permeable inhibitor of HIF-1-mediated gene transcription
A14404 SALE	Molidustat	HIF-PH 抑制剂	Molidustat is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells.
A14319 SALE	PX-478 HCl	HIF-1alpha 抑制剂	PX-478 is HIF-1alpha inhibitor, is also an orally active small molecule with potential antineoplastic activity. PX-478 has excellent activity against established human tumor xenografts, providing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. PX-478 is a highly water soluble molecule, with good i.v., i.p. and p.o. antitumor activity.
A12978 SALE	BAY 87-2243	HIF 抑制剂	BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I.
A12921	HIF-C2	HIF-2 抑制剂	HIF-C2 is a potent and selective allosteric inhibitor of hypoxia inducible factor-2 (HIF-2)
A12883	FM19G11	HIF?? 抑制剂	FM19G11 is an inhibitor of Hypoxia Inducible Factors α (HIFα), which are transcription factors that respond to changes in available oxygen in the cellular environment.
A11924 SALE	IOX 2	HIF-PHD 抑制剂	IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. Product Citations (1) Mun Chiang Chan, etc. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015; 10(7): e0132004.
A11237 SALE	FG-4592 (Roxadustat)	HIF-PHs 抑制剂	FG-4592 is a novel hypoxia inducible factor prolyl hydroxylase inhibitor, in CKD anemia. Product Citations (3) Hideaki Nakamura, .et al. Differentiated embryo chondrocyte plays a crucial role in DNA damage response via transcriptional regulation under hypoxic conditions, PLoS One, 2018, 13(2): e0192136 PMID: 29466367 Singh C, .et al. 3-Hydroxypyruvate Destabilizes Hypoxia Inducible Factor and Induces Angiostasis, Invest Ophthalmol Vis Sci, 2018, Jul 2;59(8):3440-3448 PMID: 30025089 George Hoppe, .et al. Comparative systems pharmacology of HIF stabilization in the prevention of retinopathy of prematurity, Proc Natl Acad Sci U S A, 2016, May 3; 113(18): E2516每E2525 PMID: 27091985
A16181	HIF-2a Translation Inhibitor	HIF-2a translation 抑制剂	HIF-2a translation inhibitor (IC50 value 5 uM); Decreases HIF-2a protein and HIF-2a target gene expression in normoxia and hypoxia independent of HIF-2a mRNA expression or HIF-2a protein stability, and independent of mTOR activity. Moreover, the translation inhibitor 76 enhances binding of IRP1 to the HIF-2a IRE (Iron-Responsive Element).

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A15358

A15360

A15359 SALE

A15895

A12671 SALE

A15793 SALE

A15530 SALE

A14367

A10012 SALE

A14021

A14404 SALE

A14319 SALE

A12978 SALE

A12921

A12883

A11924 SALE

A11237 SALE

A16181