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Hydroxylation

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (2) Autophagy (2) Bacterial (2) Biochemical Assay Reagents (1) Cytochrome P450 (8) Drug Metabolite (2) Endogenous Metabolite (1) Fungal (2) HIF/HIF Prolyl-Hydroxylase (1) Isotope-Labeled Compounds (1) Na+/K+ ATPase (1) RAR/RXR (2) VD/VDR (1)
By Research Areas:	Cancer (8) Cardiovascular Disease (1) Infection (4) Inflammation/Immunology (5) Metabolic Disease (5) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-106019C

Liarozole dihydrochloride R75251 dihydrochloride	Cytochrome P450 RAR/RXR	Metabolic Disease Inflammation/Immunology Cancer
Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC₅₀=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties .

HY-106019

Liarozole R75251	Cytochrome P450 RAR/RXR	Metabolic Disease Inflammation/Immunology Cancer
Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC₅₀=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties .

HY-W025062

Diethyl pyridine-2,4-dicarboxylate	Others	Others
Diethyl pyridine-2,4-dicarb is a potent prolyl 4-hydroxylase-directed proinhibitor. Diethyl pyridine-2,4-dicarb inhibits prolyl hydroxylation and procollagen processing in chick-embryo calvaria .

HY-N2586

Tenuifoliside C

Others Inflammation/Immunology

Tenuifoliside C, isolated from polygala tenuifolia willd, significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 .

Tenuifoliside C	Others	Inflammation/Immunology
Tenuifoliside C, isolated from polygala tenuifolia willd, significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 .

HY-Y0850O

Polyvinyl alcohol (Mw 31000-50000, 87-89% hydrolyzed) PVA (Mw 31000-50000, 87-89% hydrolyzed); Poly(Ethenol) (Mw 31000-50000, 87-89% hydrolyzed)	Biochemical Assay Reagents	Others
Polyvinyl alcohol (Mw 31000-50000, 87-89% hydrolyzed) is a synthetic polymer derived from polyvinyl acetate through partial or complete hydroxylation .

HY-N1407

Polygalaxanthone III
Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC₅₀ of 50.56 μM .

HY-129731

Lappaconine

Others Others

Lappaconine is a diterpenoid alkaloid. Lappaconine can be used for α-hydroxylation of β-oxo esters .

Lappaconine	Others	Others
Lappaconine is a diterpenoid alkaloid. Lappaconine can be used for α-hydroxylation of β-oxo esters .

HY-135560

Nicotelline Nicotellin	Cytochrome P450	Neurological Disease
Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke .

HY-N7697E

Chitotriose trihydrochloride	Others	Others
Chitotriose trihydrochloride is an orally active chitooligosaccharide with antioxidant activities. Chitotriose trihydrochloride inhibits hydroxylation of benzoate to salicylate by H₂O₂ in the presence of Cu ²⁺ (IC₅₀ value of 80 μM) .

HY-N9434

5,7,2',6'-Tetrahydroxyflavone	Cytochrome P450	Metabolic Disease
5,7,2',6'-Tetrahydroxyflavone is a natural flavonoid that inhibits hepatic testosterone 6β-hydroxylation (CYP3A4) activity with an IC₅₀ of 7.8 μM .

HY-113025A

L-hydroxylysine dihydrochloride (2S,5R)-5-Hydroxylysine dihydrochloride	Endogenous Metabolite	Others
L-hydroxylysine dihydrochloride ((2S,5R)-5-Hydroxylysine dihydrochloride), an amino acid, is exclusive to collagen protein, which is formed by posttranslational hydroxylation of some lysine residues .

HY-111975

*7'-Hydroxy* ABA** 7'-OH ABA	Others	Metabolic Disease
7'-Hydroxy ABA (7'-OH ABA) is a metabolite of Abscisic acid (Abscisic acid) through hydroxylation of the 7′-carbon atom of Abscisic acid. 7'-Hydroxy ABA exhibits significant hormonal activity .

HY-33549

α-Methyl-p-tyrosine
α-Methyl-p-tyrosine is a competitive inhibitor of the enzyme tyrosine hydroxylase, which converts tyrosine to Levodopa (DOPA). α-Methyl-p-tyrosine is an orally active inhibitor of catecholamine synthesis which inhibits the hydroxylation of tyrosine to DOPA .

HY-N11676

*6-Hydroxy-TSU-68*	Drug Metabolite	Cancer
6-Hydroxy-TSU-68 is a derivative of TSU-68 (HY-10517). It is a metabolite of the biotransformation pathway of TSU-68 in human liver microsomes. The content represents the self-induced hydroxylation level of TSU-68 .

HY-N11677

*7-Hydroxy-TSU-68*	Drug Metabolite	Others
7-Hydroxy-TSU-68 is a derivative of TSU-68 (HY-10517). It is a metabolite of the biotransformation pathway of TSU-68 in human liver microsomes. The content represents the self-induced hydroxylation level of TSU-68 .

HY-116444A

16-HETE	Na+/K+ ATPase	Cardiovascular Disease Inflammation/Immunology
16-HETE is arachidonic acid metabolite through subterminal hydroxylation by cytochrome P-450. 16-HETE exhibits vasodilatory and PMN inhibitory effects and serves as biomarker for early stages of non-alcoholic fatty liver disease .

HY-15439

(24S)-24,25-Dihydroxyvitamin D3 (24S)-24,25-Dihydroxycholecalciferol	VD/VDR	Others
(24S)-24,25-Dihydroxyvitamin D3 ((24S)-24,25-Dihydroxycholecalciferol) is an inactive form of vitamin D3 which undergoes various levels of hydroxylation to form active vitamin D3 analogs.

HY-17508

Clarithromycin Maximum Cited Publications 11 Publications Verification	Bacterial Cytochrome P450 Autophagy Antibiotic	Infection Cancer
Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-121172

1,4-DPCA 1 Publications Verification	HIF/HIF Prolyl-Hydroxylase	Cancer
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC₅₀ of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC₅₀ of 60 μM .

HY-153394

Aflatoxin Q1	Fungal	Infection
Aflatoxin Q1 is a hydroxy metabolite of Aflatoxin B1 (AFB1), which is a mycotoxin produced by Aspergillus flavus (A. flavus). Aflatoxin Q1, as well as and aflatoxin B1 8,9-oxide, is the major oxidative products formed from aflatoxin B1 in human liver microsomes, at all substrate concentrations. the 3 alpha-hydroxylation of aflatoxin B1 to aflatoxin Q1 is a potentially significant detoxication pathway .

HY-17508S1

Clarithromycin-d3	Isotope-Labeled Compounds	Others
Clarithromycin-d₃is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-17508R

Clarithromycin (Standard)	Bacterial Cytochrome P450 Autophagy Antibiotic	Infection Cancer
Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-100991

FG 7142 ZK 39106; LSU-65
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (K_i=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC₅₀= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .

HY-155141

hCYP3A4-IN-1	Cytochrome P450	Cancer
hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC₅₀ values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .

HY-N2071

Cedrol 1 Publications Verification (+)-Cedrol; α-Cedrol	Cytochrome P450 Fungal	Infection Inflammation/Immunology Cancer
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with K_i of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library	2507 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 2507 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

2507 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 2507 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.

Polyvinyl alcohol (Mw 31000-50000, 87-89% hydrolyzed) PVA (Mw 31000-50000, 87-89% hydrolyzed); Poly(Ethenol) (Mw 31000-50000, 87-89% hydrolyzed)	Drug Delivery
Polyvinyl alcohol (Mw 31000-50000, 87-89% hydrolyzed) is a synthetic polymer derived from polyvinyl acetate through partial or complete hydroxylation .

*N-((RS)-2-Hydroxy-propyl)-Val-Leu-anilide*	Peptides	Others
N-((RS)-2-Hydroxy-propyl)-Val-Leu-anilide is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .

LPPM-8	Peptides	Others
LPPM-8 is a ligand of Med25 and an inhibitor of Med25 protein-protein interactions (PPIs). LPPM-8 engages Med25 through interaction with the H2 face of its Activator Interaction Domain and stabilizes full-length protein in the cellular proteome. LPPM-8 is an orthosteric inhibitor of H2-binding transcriptional activators (such as ATF6a). LPPM-8 can be used for studying Med25 and Mediator complex biology .

Ternatin	Peptides	Metabolic Disease
Ternatin (compound 2) is a cyclic heptapeptides that can be isolated from mushroom Coliorus versicolor. Ternatin inhibits fat-accumulation with an IC₅₀ of 0.027 μM in 3T3-L1 adipocytes .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2586

Tenuifoliside C	Monophenols Classification of Application Fields Simple Phenylpropanols Source classification Polygalaceae Phenols Phenylpropanoids Plants Disease Research Fields Inflammation/Immunology Polygala tenuifolia Willd.	Others
Tenuifoliside C, isolated from polygala tenuifolia willd, significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 .

HY-129731

Lappaconine	Structural Classification Alkaloids Aconitum septentrionale Koelle Other Alkaloids Source classification Ranunculaceae Plants	Others
Lappaconine is a diterpenoid alkaloid. Lappaconine can be used for α-hydroxylation of β-oxo esters .

HY-N7697E

Chitotriose trihydrochloride	Polysaccharides Microorganisms Classification of Application Fields Source classification Other Diseases Disease Research Fields Saccharides	Others
Chitotriose trihydrochloride is an orally active chitooligosaccharide with antioxidant activities. Chitotriose trihydrochloride inhibits hydroxylation of benzoate to salicylate by H₂O₂ in the presence of Cu ²⁺ (IC₅₀ value of 80 μM) .

HY-N9434

5,7,2',6'-Tetrahydroxyflavone	Flavonoids Dalbergia odorifera T. Chen Flavones Leguminosae Plants	Cytochrome P450
5,7,2',6'-Tetrahydroxyflavone is a natural flavonoid that inhibits hepatic testosterone 6β-hydroxylation (CYP3A4) activity with an IC₅₀ of 7.8 μM .

HY-113025A

L-hydroxylysine dihydrochloride (2S,5R)-5-Hydroxylysine dihydrochloride	Classification of Application Fields Ketones, Aldehydes, Acids Source classification Other Diseases Endogenous metabolite Disease Research Fields	Endogenous Metabolite
L-hydroxylysine dihydrochloride ((2S,5R)-5-Hydroxylysine dihydrochloride), an amino acid, is exclusive to collagen protein, which is formed by posttranslational hydroxylation of some lysine residues .

HY-N11676

*6-Hydroxy-TSU-68*	Structural Classification Alkaloids Monophenols Pyrrole Alkaloids Source classification Phenols Endogenous metabolite	Drug Metabolite
6-Hydroxy-TSU-68 is a derivative of TSU-68 (HY-10517). It is a metabolite of the biotransformation pathway of TSU-68 in human liver microsomes. The content represents the self-induced hydroxylation level of TSU-68 .

HY-N11677

*7-Hydroxy-TSU-68*	Structural Classification Alkaloids Monophenols Pyrrole Alkaloids Source classification Phenols Endogenous metabolite	Drug Metabolite
7-Hydroxy-TSU-68 is a derivative of TSU-68 (HY-10517). It is a metabolite of the biotransformation pathway of TSU-68 in human liver microsomes. The content represents the self-induced hydroxylation level of TSU-68 .

HY-N2071

Cedrol 1 Publications Verification (+)-Cedrol; α-Cedrol	Cedrus deodara (Roxburgh) G. Don Classification of Application Fields Pinaceae Terpenoids Sesquiterpenes Source classification Plants Inflammation/Immunology Disease Research Fields Cancer	Cytochrome P450 Fungal
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with K_i of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .

Cat. No.	Product Name	Chemical Structure

HY-17508S1

Clarithromycin-d3
Clarithromycin-d₃is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

Clarithromycin-d3

Clarithromycin-d₃is the deuterium labeledClarithromycin(HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

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Hydroxylation

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

NaturalProducts

Isotope-Labeled Compounds

Natural
Products