Tyrosine Hydroxylase

TyrH, TH

Tyrosine hydroxylase (TyrH, TH) is a rate-limiting enzyme in catecholamine biosynthesis and belongs to the family of aromatic amino acid hydroxylases. Tyrosine hydroxylase uses tetrahydrobiopterin and molecular oxygen to convert tyrosine to dopamine. The amino-terminal 150 amino acids of tyrosine hydroxylase form a domain whose structure is involved in regulating the activity of the enzyme. Regulation involves phosphorylation by multiple kinases on 4 different serine residues and dephosphorylation by 2 phosphatases. Tyrosine hydroxylase is inhibited by catecholamine neurotransmitters in a feedback manner. Dopamine competes with tetrahydrobiopterin for binding to tyrosine hydroxylase and interacts with the R domain. Tyrosine hydroxylase activity is regulated by protein-protein interactions with enzymes in the same pathway or the tetrahydrobiopterin pathway, structural proteins that are thought to be chaperones in mediating the oxidative state of neurons, and proteins that transfer dopamine to secretory vesicles. Tyrosine hydroxylase is modified in the presence of NO. Tyrosine hydroxylase expression maintains dopamine synthesis. Tyrosine hydroxylase is severely lost in Parkinson's disease and slightly lost in Alzheimer's disease.

References:

[1]. Daubner SC, et al. Tyrosine hydroxylase and regulation of dopamine synthesis. Arch Biochem Biophys. 2011 Apr 1;508(1):1-12. [Content Brief]

[2]. Zhu Y, et al. Overview of tyrosine hydroxylase in Parkinson's disease. CNS Neurol Disord Drug Targets. 2012 Jun 1;11(4):350-8. [Content Brief]

[3]. Torack RM, et al. Tyrosine hydroxylase-like (TH) immunoreactivity in Parkinson's disease and Alzheimer's disease. J Neural Transm Park Dis Dement Sect. 1992;4(2):165-71. [Content Brief]

Tyrosine Hydroxylase Related Products (12):

By Effects:	Inhibitors (9) Substrate (1) Activator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-33549

α-Methyl-p-tyrosine	Inhibitor	99.41%
α-Methyl-p-tyrosine is a competitive inhibitor of tyrosine hydroxylase, which converts tyrosine into DOPA. α-Methyl-p-tyrosine is also an orally active inhibitor of catecholamine synthesis, inhibiting the hydroxylation of tyrosine into DOPA. α-Methyl-p-tyrosine can be used in research related to epilepsy, glaucoma, cancer, and other related diseases.

HY-W013407

α-Methyltyrosine methyl ester hydrochloride	Inhibitor	98.91%
α-Methyltyrosine methyl ester hydrochloride is an orally active and competitive tyrosine hydroxylase inhibitor. α-Methyltyrosine methyl ester hydrochloride can inhibit the conversion of tyrosine to dopamine. α-Methyltyrosine methyl ester hydrochloride causes kidney damage and urethral calculi in rats. α-Methyltyrosine methyl ester hydrochloride can be used as a tool for sympathetic nervous system research.

HY-B0927

Hydrastine	Inhibitor	99.57%
Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) is a selective competitive inhibitor of tyrosine hydroxylase (TH), inhibiting dopamine biosynthesis (IC₅₀=20.7 μM, PC12 cells). Hydrastine also inhibits the organic cation transporter OCT1 (IC₅₀=6.6 μM). Hydrastine may cause neuronal toxicity through mitochondrial dysfunction rather than oxidative stress damage, and can aggravate cell apoptosis when combined with L-DOPA. Hydrastine can be used to study Parkinson's disease-related dopaminergic neuronal damage.

HY-123468

HA-1004	Inhibitor	99.04%
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models.

HY-127023

Eicosapentaenoyl serotonin	Inhibitor	99.0%
Eicosapentaenoyl serotonin (EPA-5-HT) is an endogenous fatty acid-serotonin conjugate lipid mediator. Eicosapentaenoyl serotonin acts as an inhibitor of fatty acid amide hydrolase (FAAH). Eicosapentaenoyl serotonin suppresses IL-17 release in Concanavalin A (HY-P2149)-stimulated human peripheral blood mononuclear cells. Eicosapentaenoyl serotonin is regulated by polyunsaturated fatty acids and modulates intestinal immunity and Th17 signaling. Eicosapentaenoyl serotonin can be used for the study of inflammatory bowel disease-related mechanisms.

HY-182893

SK-129	Activator
SK-129 is a blood-brain barrier-permeable inhibitor of α-synuclein (αS) oligomers with a K_d of 221 nM. SK-129 preferentially binds to neurotoxic αS oligomers over physiological αS monomers, inhibits αS aggregation, blocks the interaction and co-aggregation of αS with tau protein, and prevents the maturation of αS-tau condensates into amyloid aggregates. SK-129 reduces ROS production, rescues dopaminergic neuron degeneration, improves motor function, restores endogenous dopamine synthesis, increases the number of Tyrosine Hydroxylase-positive neurons, prevents brain histopathological changes, alleviates neuroinflammation, and improves survival rates in relevant models. SK-129 can be used in research related to Parkinson's disease (PD) and Lewy body dementia (LBD).

HY-103439A

GW583340	Inhibitor
GW583340 (compound 6) is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW583340 exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW583340 is applicable to research related to head and neck cancer, breast cancer, and gastric cancer.

HY-175149

2-Fluorodeoxyarbutin	Inhibitor
2-Fluorodeoxyarbutin, a derivative of Deoxyarbutin (HY-B1461), is a tyrosine hydroxylase and dopa oxidase inhibitor. 2-Fluorodeoxyarbutin inhibits melanin synthesis in intact melanocytes. 2-Fluorodeoxyarbutin can be used for the strudy of skin lightening or for ameliorating hyperpigmented lesions.

HY-150100

Tyrosine 3-monooxygenase
Tyrosine 3-monooxygenase (Tyrosine hydroxylase) is a rate-limiting enzyme in catecholamine biosynthesis and belongs to the family of aromatic amino acid hydroxylases. Tyrosine 3-monooxygenase catalyzes the initial and rate-limiting step in the biosynthetic pathway of catecholamines, including dopamine, noradrenaline, and adrenaline.

HY-137838

H-Tyr-AMC	Substrate
H-Tyr-AMC is a fluorogenic substrate for tyrosine aminopeptidases. H-Tyr-AMC is an inhibitor of tobacco and potato hydroxycinnamoyl-CoA:tyramine N-(hydroxycinnamoyl)transferase (THT) with K_i values of 0.72 μM (tobacco) and 0.42 μM (potato).

HY-33549R

α-Methyl-p-tyrosine (Standard)	Inhibitor
α-Methyl-p-tyrosine (Standard) is the analytical standard of α-Methyl-p-tyrosine. This product is intended for research and analytical applications. α-Methyl-p-tyrosine is a competitive inhibitor of tyrosine hydroxylase, which converts tyrosine into DOPA. α-Methyl-p-tyrosine is also an orally active inhibitor of catecholamine synthesis, inhibiting the hydroxylation of tyrosine into DOPA. α-Methyl-p-tyrosine can be used in research related to epilepsy, glaucoma, cancer, and other related diseases.

HY-B0927R

Hydrastine (Standard)	Inhibitor
Hydrastine (Standard) is the analytical standard of Hydrastine (HY-B0927). This product is intended for research and analytical applications. Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) is a selective competitive inhibitor of tyrosine hydroxylase (TH), inhibiting dopamine biosynthesis (IC₅₀=20.7 μM, PC12 cells). Hydrastine also inhibits the organic cation transporter OCT1 (IC₅₀=6.6 μM). Hydrastine may cause neuronal toxicity through mitochondrial dysfunction rather than oxidative stress damage, and can aggravate cell apoptosis when combined with L-DOPA. Hydrastine can be used to study Parkinson's disease-related dopaminergic neuronal damage.

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