hydroxylase

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.

Collagen proline hydroxylase inhibitor-1 exhibits antifibroproliferative activity.

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.

Collagen proline hydroxylase inhibitor is an inhibitor collagen proline hydroxylase and useful for antifibrotic proliferative agents.

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

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].

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.

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.

Casein is a milk protein with multiple roles in a novel drug delivery system that affects postprandial amino acid delivery in different ways through its intragastric coagulation properties.

Sapropterin dihydrochloride (6R-BH4 dihydrochloride) is phenylalanine hydroxylase agonist that is approved for the treatment of BH4 responsive PKU.

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), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

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

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

SU 10603 is a specific inhibitor of 17α-hydroxylase (also known as CYP17A1 and P450c17) used to study steroid hormone synthesis.

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH) and a concentration-dependent dual inhibitor of P-gp and BCRP, with IC50 values of 73.8 μM and 17.0 μM, respectively.

ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM[1].