HIF

Hypoxia-inducible factor 1-alpha, also known as HIF-1-alpha, is a subunit of a heterodimeric transcription factor hypoxia-inducible factor 1 (HIF-1) that is encoded by the HIF1A gene. It is a basic helix-loop-helix PAS domain containing protein, and is considered as the master transcriptional regulator of cellular and developmental response to hypoxia. The dysregulation and overexpression of HIF1A by either hypoxia or genetic alternations have been heavily implicated in cancer biology, as well as a number of other pathophysiologies, specifically in areas of vascularization and angiogenesis, energy metabolism, cell survival, and tumor invasion. Two other alternative transcripts encoding different isoforms have been identified.

カタログ番号	製品名
T10258	AFP464 free base	AFP464 (NSC710464) free base is an active HIF-1α inhibitor (IC50: 0.25 μM) and a potent aryl hydrocarbon receptor (AhR) activator.
TN4489	Manassantin A	Manassantin A is a high potent HIF-1 inhibitor, it protects the gastric mucosa from ethanol-induced acute gastric injury, and suggest that these protective effec...
TN1951	Moracin O	Moracin O shows significant neuroprotective, and analgesic activities, it also has a strong protective influence against doxorubicin-induced cardiomyopathy in H9...
T6804	Chetomin	Chetomin is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.
T13402	ZK-261991	ZK-261991 is an orally active inhibitor of VEGFR tyrosine kinase(IC50 of 5 nM, VEGFR2).
TN2040	Panaxynol	Panaxynol is the most potent antiplatelet agent in ginseng and its mechanism of action is chiefly due to the inhibition of thromboxane formation.
T12675	(Rac)-PT2399	(Rac)-PT2399 is a potent and specific inhibitor of hypoxia-inducible factor 2a (HIF-2α)(IC50 of 0.01 μM).
TN4603	Myricanol	Myricanol can elicit growth inhibitory and cytotoxic effects on lung cancer cells, it can significantly decelerate tumor growth in vivo by inducing apoptosis.
T15234	ENMD-1198	ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
TN5250	Vomifoliol	Vomifoliol is most likely the immediate precursor of dehydrovomifoliol, because of the organism converted abscisic acid (ABA), to dehydrovomifoliol as the major ...
TN1952	Moracin P	Moracin P exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tum...
TN2250	Syringaresinol	(-)-Syringaresinol may be a potential chemotherapeutic agent for the treatment of cancer; it against H/R-induced cardiomyocyte injury and death, the degradation ...
T11562	HIF-2α-IN-3	HIF-2α-IN-3 is an allosteric inhibitor of HIF-2α (IC50: 0.4 µM; KD: 1.1 µM) with anticancer activity.
T17009	TC-S 7009	TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd 5 μM). TC-S 7009 is an effective and selective inhibitor of HIF-2α (Kd: 81 nM). TC-S 7009 disrupts HIF-2...
T19832	Acriflavine Hydrochloride	Acriflavine Hydrochloride is a HIF-1α inhibitor. It acts by targeting HIF-1α-mediated pathways and decreasing the level of PGK1, VEGF, and HIF-1α in vitro and in...
T22022	Adaptaquin	Adaptaquin is an inhibitor of the hypoxia-inducing factor prolyl hydroxylase (HIF-PH) [1] [2].
T29797	AKB-6899	AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macr...
T10233	Acetylarenobufagin	Acetylarenobufagin is a steroidal hypoxia-inducible factor-1 (HIF-1) modulator.
T11589	Hydroxycitric acid tripotassium hydrate	Potassium citrate monohydrate effectively inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation, and anti-tumor effects. Hydr...
T13925	THS-044	THS-044 binding stabilizes the HIF2α PAS-B folded state with a kd of 2 μM and regulates HIF2 activity in endogenous and clinical settings.
T7802	M1001	M1001 is a HIF-2α agonist.
TQ0121	VH-298	VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein...
T4S1551	Cinnamaldehyde	1. Cinnamaldehyde has antipyretic activity. 2. Cinnamaldehyde is a sedative agent. 3. Cinnamaldehyde inhibits invasive capabilities of MDA-MB-435S cells was corr...
T3027	Sodium Aescinate	Sodium Aescinate is extracted from Aesculus wilsonii.
T0153	Oltipraz	Oltipraz is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as g...
T5176	Desidustat	Desidustat is an inhibitor of HIF hydroxylase.
T36711	FM19G11	FM19G11 is an inhibitor of hypoxia inducible factor (HIF) α-subunit (IC50 = 80 nM in hypoxia induced luciferase assay).
T6961	PX-478	PX-478 2HCl is an orally active, and selective inhibitor of hypoxia-inducible factor-1α (HIF-1α).
T1939	DMOG	DMOG, an antagonist of the α-ketoglutarate cofactor, is an inhibitor for HIF prolyl hydroxylase.
T5537	IDF-11774	IDF-11774 is a HIF-1 inhibitor.It reduces hif-1α HRE luciferase activity (IC50 = 3.65 μM).
T15396	GN44028	GN44028 is an inhibitor of HIF-1 (IC50: 14 nM). GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity. However, It can not be suppressing HIF-1α mRNA ...
T4S0800	Demethyleneberberine	Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either ...
T12675L	PT2399	PT2399 shows effective antitumor activity in vivo. PT2399 is an effective and selective HIF-2α antagonist, which directly binds to the HIF-2α PAS B domain (IC50:...
T7692	2,4-DPD	2,4-DPD is competitive inhibitor of the oxygen-sensing enzyme HIF-α prolyl hydroxylase (HIF-PH)
T7836	ML228	ML228 is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target ...
T6929	Pantoprazole sodium	Pantoprazole Sodium is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole is a lipophilic, weak base that cros...
T13050	SYP-5	SYP-5 is a novel inhibitor of HIF-1, suppresses tumor cells invasion and angiogenesis.
T3494	LW6	LW6 is a novel HIF-1 inhibitor.
T3169	KC7F2	KC7F2 is a potent HIF-1 pathway inhibitor with potential anti-cancer activity.
T5740	25(R,S)-Ruscogenin	(25RS)-Ruscogenin is a natual product.
T11561	HIF-2α-IN-2	HIF-2α-IN-2 is a hypoxia-inducible factor (HIF-2α) inhibitor (IC50: 16 nM in scintillation proximity assay).
T3404	Cucurbitacin B	Cucurbitacin B has profound in vitro and in vivo antiproliferative effects against human pancreatic Y cells. It inhibited AKT signaling activation through up-reg...
T16679	Belzutifan	PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC). PT2977 is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). PT2977, as a...
T7848	PT-2385	PT-2385 is a selective HIF-2α inhibitor (Kd<50 nM).
T4651	Vadadustat	Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
T9890	HIF1-IN-3	HIF1-IN-3 is an effective inhibitor of HIF-1 (EC50 = 0.9 μM) and can be used in anticancer studies.
T2389	Dapagliflozin	Dapagliflozin is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.
T2488	BAY 87-2243	BAY 87-2243 is a potent and selective inhibitor of hypoxia-inducible factor-1 (HIF-1).
T3197	Daprodustat	Daprodustat (GSK1278863) is a HIF-prolyl hydroxylase inhibitor.
TN1480	Cephaeline	Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeo...