hydroxylase

p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine HCL) is a novel, potent, and specific inhibitor of TPH[1]. Its potential to selectively and reversibly inhibit serotonin biosynthesis may contribute to characterizing the role of serotonin in behavioral and physiological activities[1].

Ro 61-8048 is a potent and selective inhibitor of kynurenine hydroxylase with an IC50 value of 37 nM.

Tetrahydropiperine (Cosmoperine) is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.

FG-2216 (YM-311) is a potent HIF-prolyl hydroxylase inhibitor for the PDH2 enzyme (IC50: 3.9 uM); orally bioavailable and induced reversible and significant Epo induction in vivo.

Cholesterol 24-hydroxylase-IN-1 is an orally active, selective, and potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) that crosses the blood-brain barrier.Cholesterol 24-hydroxylase-IN-1 may be useful in the study of epilepsy-like neurological disorders. Cholesterol 24-hydroxylase-IN-1 is used to study epilepsy-like neurological diseases.

Prolyl-4-hydroxylase Inhibitor 11, a novel proline 4-hydroxylase inhibitor, shows protective effects against oxidative stress and Cu(II) toxicity in Chlorella vulgaris.

Prolyl Hydroxylase inhibitor 1 is an orally active inhibitor of hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) (IC50 of 62.23 nM).

Cholesterol24-hydroxylase-IN-3 is an orally bioavailable, selective, brain-penetrant CH24H inhibitor (IC50 = 23 nM), classified as a 1,3-oxazole derivative. It inhibits CH24H enzyme activity competitively by coordinating the 1,3-oxazole nitrogen atom with the heme iron, with the cyclopropyl group occupying a hydrophobic pocket. Cholesterol24-hydroxylase-IN-3 has potential applications in research on neurological disorders like epilepsy.

"Lysyl Hydroxylase 2-IN-1 (compound 12) is a selective inhibitor of lysyl hydroxylase 2 (LH2) with an IC50 of approximately 300 nM and demonstrates specificity for LH2 over LH1 and LH3 [1]."

Lysyl Hydroxylase 2-IN-2 (compound 13) is a potent inhibitor of Lysyl Hydroxylase 2 (LH2), exhibiting an IC50 of approximately 500 nM. It effectively inhibits cell migration in 344SQ WT cells without affecting the migration of LH2 knockout cells [1].

Cholesterol 24-hydroxylase-IN-2, a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), exhibits an IC50 value of 5.4 nM and has potential applications in mammalian imaging of this enzyme [1].

LX-1031 is an effective inhibitor of tryptophan 5-hydroxylase. LX-1031 decreases serotonin (5-HT) synthesis peripherally.

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine), a selective, effective, and reversible tryptophan hydroxylase (TPH) inhibitor, exhibits competitive inhibition with a Ki of 32.6 μM.

Diethyl-pythiDC is an collagen prolyl 4-hydroxylase inhibitor.

Bupicomide is a dopamine beta hydroxylase inhibitor with antihypertensive and vasodilatory activity that reduces 14C-norepinephrine biosynthesis of 14C-dopamine and can be used to study hypertension.

Ketoconazole (R-41400) is an imidazole antifungal agent with broad-spectrum antifungal activity that primarily acts by inhibiting the biosynthesis of ergosterol in the fungal cell membrane. Ketoconazole inhibits the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase (CYP51), thereby blocking the conversion of lanosterol to ergosterol. This leads to damage to the cell membrane structure and permeability, consequently inhibiting fungal growth and producing an antifungal effect. In addition, ketoconazole is a non-selective cytochrome P450 (CYP) inhibitor, specifically inhibiting drug-metabolizing enzymes such as human CYP3A4. In terms of endocrinology, ketoconazole also inhibits various enzymes involved in steroid synthesis (CYP17A1, CYP11A1).

Fenclonine (CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine(CP-10188) acts pharmacologically to deplete endogenous levels of serotonin.

Mildronate (Meldonium) is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.

pCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride) is an inhibitor of tryptophan hydroxylase inhibitor and 5-HT synthesis. pCPA methyl ester hydrochloride is permeable across the blood-brain barrier and reduces 5-HT central availability.

p-Fluoro-L-phenylalanine is a substrate for tyrosine hydroxylase (TH) that can be used to study the regulation of that enzyme. p-Fluoro-L-phenylalanine binds to the L-leucine specific receptor of Escherichia coli with an KD of 0.26 μM.

Tetrahydropapaverine hydrochloride (Norlaudanosine HCl) , an analogue of salsolinol and tetrahydropapaveroline, has neurotoxicity on dopamine neurons.

Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.

4-Chloro-L-phenylalanine (L-PCPA) is an inhibitor of 5-HT biosynthesis and a non-specific antagonist of tryptophan hydroxylase (TPH1 and TPH2).