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Results for "

tumor vascularity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (6) c-Met/HGFR (2) Calcium Channel (1) CD47 (1) Endogenous Metabolite (7) ERK (1) Estrogen Receptor/ERR (1) FAK (1) HIF/HIF Prolyl-Hydroxylase (1) Histone Demethylase (4) HPV (1) IFNAR (1) Influenza Virus (1) Microtubule/Tubulin (11) Mitochondrial Metabolism (1) mTOR (1) Parasite (1) PDK-1 (1) PERK (1) Prostaglandin Receptor (2) Ras (1) Ser/Thr Protease (1) Small Interfering RNA (siRNA) (2) STAT (2) STING (1) TGF-β Receptor (1) Trk Receptor (1) VEGFR (4)
By Research Areas:	Cancer (39) Cardiovascular Disease (3) Endocrinology (3) Infection (2) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (4)
Oligonucleotides:	siRNAs (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Targets Recommended: TNF Receptor BRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-A0096

Iloprost 4 Publications Verification Ciloprost; ZK 36374	Prostaglandin Receptor Endogenous Metabolite	Cardiovascular Disease Endocrinology Cancer
Iloprost (ZK 36374; Ciloprost) is a prostacyclin (PGI2) analogue, involves in embryo development and inflammation improvement, and inhibits tumor metastasis. Iloprost can be used for peripheral vascular research .

HY-16114

BNC105 1 Publications Verification	Microtubule/Tubulin	Cancer
BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.

HY-16147

Combretastatin A1 phosphate Oxi4503; CA1P; Combretastatin A1 diphosphate	Others	Cancer
Combretastatin A1 phosphate (Oxi4503; CA1P; Combretastatin A1 diphosphate) is a potent vascular disruptive agent. Combretastatin A1 phosphate exerts anti-angiogenic effects on tumors. Combretastatin A1 phosphate has the potential for the research of pancreatic neuroendocrine tumors .

HY-P5107

Low molecular weight protamine LMWP	VEGFR	Cancer
Low molecular weight protamine is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity. Low molecular weight protamine can inhibit tumor growth and is used in cancer research .

HY-13598

Valecobulin CKD-516	Microtubule/Tubulin	Cancer
Valecobulin (CKD516) is a valine proagent of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors .

HY-117836

FAK-IN-16	FAK	Cancer
FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC₅₀ of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .

HY-A0096R

Iloprost (Standard)	Prostaglandin Receptor Endogenous Metabolite	Endocrinology Cancer
Iloprost (Standard) is the analytical standard of Iloprost. This product is intended for research and analytical applications. Iloprost (ZK 36374; Ciloprost) is a prostacyclin (PGI2) analogue, involves in embryo development and inflammation improvement, and inhibits tumor metastasis. Iloprost can be used for peripheral vascular research .

HY-14919

Denibulin MN-029 free base	Microtubule/Tubulin	Cancer
Denibulin, a novel vascular-disrupting agent, inhibits microtubule assembly reversibly, disrupting tumor vascular endothelial cell cytoskeletons. Denibulin demonstrated tolerability and potential anti-vascular effects, warranting further investigation in cancer therapy .

HY-14815

Fosbretabulin Combretastatin A4 phosphate	Apoptosis Microtubule/Tubulin	Cancer
Fosbretabulin (Combretastatin A4 phosphate) is a vascular disruptor with antitumor activity against atypical thyroid carcinoma (ATC) cell lines and xenografts. Fosbretabulin inhibits tumor growth by inhibiting microtubule polymerization, inducing apoptosis, and suppressing angiogenesis in tumors .

HY-15855

Fosbretabulin tromethamine	Others	Cancer
Fosbretabulin (tromethamine), also known as combretastatin A4 phosphate (CA4P), is a vascular disrupting agent evaluated for its efficacy against anaplastic thyroid carcinoma (ATC). It targets tumor neovasculature, causing acute and reversible reductions in tumor blood flow and central necrosis .

HY-10964

Vadimezan Maximum Cited Publications 44 Publications Verification DMXAA; ASA-404	STING IFNAR Influenza Virus	Infection Cancer
Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan has anti-influenza virus H1N1-PR8 activities.

HY-103316A

Ned 19 2 Publications Verification	Calcium Channel	Cardiovascular Disease Cancer
Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca ²⁺ signaling, with an IC₅₀ of 65 nM . Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice .

HY-13598A

Valecobulin hydrochloride CKD-516 hydrochloride	Microtubule/Tubulin	Cancer
Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine proagent of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors .

HY-153482

ATU027	Small Interfering RNA (siRNA)	Cancer
ATU027 is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.

HY-153482A

ATU027 sodium	Small Interfering RNA (siRNA)	Cancer
ATU027 sodium is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 sodium has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.

HY-136476B

Cu(II) protoporphyrin IX	Others	Inflammation/Immunology Cancer
Cu (II) Protoporphyrin IX is used as a negative control for Zn (II) Protoporphyrin (an inihibitor of heme oxygenase). Heme oxygenase has been implicated in tumor cell resistance to chemotherapy, reduction of free radical formation and inflammation, and associated with vascular repair .

HY-10338A

Foretinib phosphate	c-Met/HGFR VEGFR	Cancer
Foretinib phosphate is an orally bioavailable small molecule with potential anti-tumor activity. Foretinib phosphate can selectively inhibit hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), thereby potentially inhibiting tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib phosphate shows different anti-cancer activity from cabozantinib in lung cancer cells and has stronger inhibitory effects on targets such as MEK1/2, FER and AURKB .

HY-119618

R1498	Endogenous Metabolite	Cancer
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .

HY-14444

Plinabulin NPI-2358	Microtubule/Tubulin	Cancer
Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC₅₀ of 9.8 nM against HT-29 cells . Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells .

HY-16196

ENMD-1198 IRC-110160	Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT	Cancer
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.

HY-121993

Combretastatin A-1	Microtubule/Tubulin	Cancer
Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects .

HY-145820

Tubulin inhibitor 14	Apoptosis Microtubule/Tubulin	Cancer
Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC₅₀ of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features .

HY-157148

1D228	c-Met/HGFR Trk Receptor	Cancer
1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors .

HY-19471

(rac)-ZK-304709	Others	Cancer
(rac)-ZK-304709 is an isomer of ZK-304709. It is a first-in-class oral multi-target tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (Cdks), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. It directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. In an orthotopic BON tumor model, (rac)-ZK-304709 reduced primary tumor growth by 80% and reduced tumor microvascular density. These results suggest that (rac)-ZK-304709 can effectively control tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may be a potential agent for the treatment of NET.

HY-16146

Combretastatin A-1 phosphate tetrasodium OXi-4503 tetrasodium	Microtubule/Tubulin	Cancer
Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a proagent of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects .

HY-160853

Tubulin inhibitor 42	Apoptosis Microtubule/Tubulin	Cancer
Tubulin inhibitor 42 (Compound 14b) dose-dependently inhibited the activity of β-microtubulin (IC₅₀ = 3.5 µM).Tubulin inhibitor 42 interferes with microtubule dynamic homeostasis, resulting in the arrest of the cancer cell cycle in the G2/M phase and inducing apoptosis. Tubulin inhibitor 42 significantly inhibits the angiogenic process in vitro and in vivo, preventing vascularization and tumor growth .

HY-P10388

TAX2 peptide	CD47 TGF-β Receptor	Cancer
TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .

HY-116452

YLT192	Others	Cancer
YLT192 is an orally active and highly bioavailable VEGFR2 inhibitor with potent anti-angiogenic activity and anti-tumor efficacy. YLT192 significantly inhibited the kinase activity of VEGFR2 and inhibited the proliferation, migration, invasion and tube formation of human umbilical cord vascular endothelial cells. YLT192 also inhibited VEGF-induced VEGFR2 phosphorylation and its downstream signaling regulators. YLT192 also showed the ability to inhibit angiogenesis in vivo in zebrafish embryo models and alginate-coated tumor cell experiments. YLT192 can directly inhibit the proliferation of cancer cells and induce their apoptosis .

HY-12018A

Vatalanib hydrochloride PTK787 hydrochloride; ZK-222584 hydrochloride; CGP-797870 hydrochloride	VEGFR Apoptosis	Others Cancer
Vatalanib (PTK787; ZK-222584; CGP-797870) hydrochloride is an inhibitor of VEGFR2/KDR with an IC₅₀ of 37 nM .

HY-124379

TPCK 1 Publications Verification L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK	Ser/Thr Protease HPV Apoptosis PDK-1	Infection Neurological Disease Inflammation/Immunology Cancer
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats .

HY-163712

17-Epiestriol	Estrogen Receptor/ERR	Endocrinology
17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase .

HY-164551

YLL545	VEGFR STAT ERK Apoptosis	Cancer
YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth .

HY-117807

A-176120	Ras	Cancer
A-176120 is a potent inhibitor of farnesyltransferase, crucial for Ras protein farnesylation in cancer cells. It exhibits high selectivity for farnesyltransferase (IC₅₀ 1.2 ± 0.3 nM) over related enzymes like geranylgeranyltransferases and squalene synthase. Inhibition of Ras processing in H-ras and K-ras mutated cells demonstrates its efficacy in blocking Ras-mediated signaling. A-176120 shows anti-angiogenic effects by inhibiting vascular endothelial growth factor (VEGF) secretion and disrupting capillary formation in endothelial cells. In vivo studies reveal its ability to reduce tumor growth in Ras-transformed cells and enhance survival in animal models. These findings highlight A-176120 as a promising FPP analogue with potent anti-tumor and anti-angiogenic properties .

HY-157231A

HC-5404-Fu	PERK	Cancer
HC-5404-Fu is a PERK inhibitor with an antitumor activity. HC-5404-Fu inhibits endoplasmic reticulum stress response signalling. HC-5404-Fu sensitizes renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). HC-5404-Fu is promising for research of renal cell carcinoma, gastric cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors .

HY-B0660

Eicosapentaenoic Acid 10+ Cited Publications EPA; Timnodonic acid	Endogenous Metabolite Histone Demethylase	Neurological Disease Cancer
Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-W011269

Eicosapentaenoic Acid sodium EPA sodium; Timnodonic acid sodium	Endogenous Metabolite Histone Demethylase	Cardiovascular Disease Metabolic Disease Cancer
Eicosapentaenoic Acid (EPA)sodium is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid sodium exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid sodium activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid sodium can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-B0660A

Eicosapentaenoic acid (metformin) EPA (metformin); Timnodonic acid (metformin)	Endogenous Metabolite Histone Demethylase	Neurological Disease Cancer
Eicosapentaenoic Acid (EPA) metformin is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic acid metformin exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). EEicosapentaenoic acid metformin activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic acid metformin can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-B0660R

Eicosapentaenoic Acid (Standard)	Endogenous Metabolite Histone Demethylase	Neurological Disease Cancer
Eicosapentaenoic Acid (Standard) is the analytical standard of Eicosapentaenoic Acid. This product is intended for research and analytical applications. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .

HY-B0263S

Thiabendazole-d4 2-(4-Thiazolyl)benzimidazole-d₄	Mitochondrial Metabolism Parasite	Others
Thiabendazole-d₄ is a deuterated form of Thiabendazole, which is an antiseptic, antifungal and antiparasitic agent[1].

HY-155721

22-(4′-py)-JA 22-(4′-Pyridinecarbonyl) jorunnamycin A	Akt mTOR	Cancer
22-(4′-py)-JA is a semisynthetic derivative of junamycin A (JA) that can be isolated from the Thai blue sponge (Xestospongia sp.). 22-(4′-py)-JA has antimetastatic activity and can inhibit AKT/mTOR/p70S6K signaling. 22-(4′-py)-JA inhibits tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC), downregulates metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α) and vascular endothelial growth factor (VEGF). 22-(4′-py)-JA has potent anticancer activity against non-small cell lung cancer (NSCLC) .

HY-13590

CEP-7055	Others	Cancer
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library	2,691 compounds
Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression. Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival. HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation. MCE offers a unique collection of 2,691 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Oxygen Sensing Compound Library

2,691 compounds

Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

MCE offers a unique collection of 2,691 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Cat. No.	Product Name	Target	Research Area