HIF-1α transcription activity

By Targets:	HIF/HIF Prolyl-Hydroxylase (13) Akt (3) Antibiotic (5) Apoptosis (3) Autophagy (3) Bacterial (3) Beclin1 (3) E1/E2/E3 Enzyme (1) Histone Acetyltransferase (1) HSP (1) JNK (3) Ligands for E3 Ligase (1) Microtubule/Tubulin (2) MMP (3) Parasite (2) Reference Standards (2) VEGFR (6)
By Research Areas:	Cancer (12) Infection (4)

Targets Recommended: HIF/HIF Prolyl-Hydroxylase Microphthalmia Associated Transcription Factor (MITF) OLIG2 ATF6 RUNX

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0239

Chloramphenicol 15+ Cited Publications	Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase VEGFR Autophagy Apoptosis Beclin1 JNK Akt MMP	Infection Cancer
Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .

HY-B0413

Fenbendazole 5+ Cited Publications	Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic	Infection Cancer
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator *HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity* and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .

HY-110266

GN44028 5+ Cited Publications	HIF/HIF Prolyl-Hydroxylase	Cancer
GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC₅₀ of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers .

HY-156106

VHL-IN-1	HIF/HIF Prolyl-Hydroxylase Ligands for E3 Ligase E1/E2/E3 Enzyme	Cancer
VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a K_d value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of *HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α* and hydroxylated *HIF-1α, and induces the transcriptional* activity of *HIF-1α*. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research .

HY-P10426

cyclo(CLLFVY)	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC₅₀ of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .

HY-B0239R

Chloramphenicol (Standard)	Reference Standards Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase VEGFR Autophagy Apoptosis Beclin1 JNK Akt MMP	Infection Cancer
Chloramphenicol (Standard) is the analytical standard of Chloramphenicol. This product is intended for research and analytical applications. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .

HY-B0413R

Fenbendazole (Standard)	Reference Standards Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic	Infection
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator *HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity* and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .

HY-123009

KCN1	HIF/HIF Prolyl-Hydroxylase Histone Acetyltransferase	Cancer
KCN1 is a *p300/HIF-1α* interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest .

HY-B0239S2

Threo-Chloramphenicol-d6	JNK Apoptosis VEGFR MMP Bacterial Akt Autophagy HIF/HIF Prolyl-Hydroxylase Antibiotic Beclin1	Cancer
Threo-Chloramphenicol-d₆ is the deuterium labeled Chloramphenicol . Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .

HY-D2360

O-Carboranylphenoxyacetanilide	HIF/HIF Prolyl-Hydroxylase HSP	Cancer
O-Carboranylphenoxyacetanilide is a *HIF-1α* inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC₅₀: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity .

HY-N10330

7-Hydroxyneolamellarin A	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer .

HY-165413

KST012174 hydrochloride	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
KST012174 hydrochloride is a potent *HIF-1α-p300/CBP* interaction inhibitor with an IC₅₀ of 107 μM. KST012174 hydrochloride completely blocks the binding of *HIF-1α* to p300 protein at a concentration of 100 μM, without affecting the expression stability of *HIF-1α* protein itself. By directly interfering with the binding between the C-terminal transactivation domain (C-TAD) of *HIF-1α* and the CH1 domain of p300, KST012174 inhibits the transcriptional activation function of HIF-1α, thereby significantly downregulating the mRNA expression level of its downstream target gene VEGF and exerting core activity in inhibiting tumor angiogenesis. KST012174 hydrochloride is applicable for research on cancer occurrence and development as well as hypoxia pathway-targeted strategies .

HY-183583

HIF-2α-IN-18	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-2α-IN-18 is a selective *HIF-2α* inhibitor with a human IC₅₀ of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the *HIF-2α/ARNT* dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting *HIF-1α* target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma^[1].

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library	4,097 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 4,097 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

4,097 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 4,097 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	Type

HY-D2360

O-Carboranylphenoxyacetanilide	Fluorescent Dyes
O-Carboranylphenoxyacetanilide is a *HIF-1α* inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC₅₀: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity .

Cat. No.	Product Name	Target	Research Area

HY-P10426

cyclo(CLLFVY)	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC₅₀ of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0239

Chloramphenicol 15+ Cited Publications	Structural Classification Classification of Application Fields Anti-aging Antibacterial Disease Research Endogenous metabolite Other Antibiotics Infection Human Gut Microbiota Metabolites Plant Cell Culture Microorganisms Antibiotics Resistance Selection Animal Husbandry Anticancer Disease Research Fields Source Classification Cancer	Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase VEGFR Autophagy Apoptosis Beclin1 JNK Akt MMP
Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .

HY-B0239R

Chloramphenicol (Standard)	Structural Classification Antibacterial Disease Research Endogenous metabolite Other Antibiotics Human Gut Microbiota Metabolites Plant Cell Culture Microorganisms Antibiotics Resistance Selection Animal Husbandry Anticancer Source Classification	Reference Standards Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase VEGFR Autophagy Apoptosis Beclin1 JNK Akt MMP
Chloramphenicol (Standard) is the analytical standard of Chloramphenicol. This product is intended for research and analytical applications. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .

HY-N10330

7-Hydroxyneolamellarin A	Animals Phenols Source Classification	HIF/HIF Prolyl-Hydroxylase VEGFR
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer .

Cat. No.	Product Name	Chemical Structure

HY-B0239S2

Threo-Chloramphenicol-d6
Threo-Chloramphenicol-d₆ is the deuterium labeled Chloramphenicol . Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .

Threo-Chloramphenicol-d6

Threo-Chloramphenicol-d₆ is the deuterium labeled Chloramphenicol . Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .

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