Hydroxylase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Hydroxylase Products

Catalog No. Information Product Use Citations Product Validations
S2695

Nepicastat (SYN-117) HCl

Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.
S4130

Mildronate

Mildronate is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.
Cancer Discov, 2020, CD-20-0288
S4586

4-Chloro-DL-phenylalanine

4-Chloro-DL-phenylalanine (Fenclonine, PCPA, CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). 4-Chloro-DL-phenylalanine acts pharmacologically to deplete endogenous levels of serotonin.
S7456

Osilodrostat (LCI699)

LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase, an enzyme catalyzing the final step of cortisol synthesis.
S6109

H-HoArg-OH

H-HoArg-OH (L-Homoarginine) is an organ-specific, uncompetitive inhibitor of human liver and bone alkaline phosphohydrolases.
S4926

(R)-Nepicastat HCl

(R)-Nepicastat HCl, the R-enantiomer of Nepicastat HCl, is a potent and selective inhibitor with IC50 of 25.1 nM and 18.3 nM for bovine and human dopamine-β-hydroxylase, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.
S5797

Metyrosine

Metyrosine, an antihypertensive drug, is a tyrosine hydroxylase inhibitor.
S8172

Ro 61-8048

Ro 61-8048 is a high-affinity kynurenine 3-hydroxylase (KMO) inhibitor with IC50 and Ki of 37 nM and 4.8 nM, respectively.
J Neurosci Res, 2020, 98(1):155-167
Leukemia, 2019, 10.1038/s41375-019-0558-x
S6044

H-Tyr(3-I)-OH

H-Tyr(3-I)-OH is responsible for catalyzing the first step of the noradrenergic biosynthesis pathway. H-Tyr(3-I)-OH is an effective tyrosine hydroxylase inhibitor.
S7483

DMOG

DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.
Cell Death Differ, 2020, 20
Cells, 2020, 9(3)
Int Immunopharmacol, 2020, 1;83:106438
S2173

Telotristat Etiprate (LX 1606 Hippurate)

Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Phase 3.
S2367

Tetrahydropapaverine HCl

Tetrahydropapaverine (Norlaudanosine), one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.
S1379

Isotretinoin

Isotretinoin (13-cis retinoic acid) was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.
Oncogene, 2020, 39(21):4212-4226
S9568

Sapropterin Dihydrochloride

Sapropterin Dihydrochloride, a synthetic preparation of the dihydrochloride salt of naturally occurring tetrahydrobiopterin (BH4), is a phenylalanine hydroxylase activator.
Catalog No. Information Product Use Citations Product Validations
S2695

Nepicastat (SYN-117) HCl

Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.
S4130

Mildronate

Mildronate is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.
Cancer Discov, 2020, CD-20-0288
S4586

4-Chloro-DL-phenylalanine

4-Chloro-DL-phenylalanine (Fenclonine, PCPA, CP-10188) is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). 4-Chloro-DL-phenylalanine acts pharmacologically to deplete endogenous levels of serotonin.
S7456

Osilodrostat (LCI699)

LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase, an enzyme catalyzing the final step of cortisol synthesis.
S6109

H-HoArg-OH

H-HoArg-OH (L-Homoarginine) is an organ-specific, uncompetitive inhibitor of human liver and bone alkaline phosphohydrolases.
S4926

(R)-Nepicastat HCl

(R)-Nepicastat HCl, the R-enantiomer of Nepicastat HCl, is a potent and selective inhibitor with IC50 of 25.1 nM and 18.3 nM for bovine and human dopamine-β-hydroxylase, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.
S5797

Metyrosine

Metyrosine, an antihypertensive drug, is a tyrosine hydroxylase inhibitor.
S8172

Ro 61-8048

Ro 61-8048 is a high-affinity kynurenine 3-hydroxylase (KMO) inhibitor with IC50 and Ki of 37 nM and 4.8 nM, respectively.
J Neurosci Res, 2020, 98(1):155-167
Leukemia, 2019, 10.1038/s41375-019-0558-x
S6044

H-Tyr(3-I)-OH

H-Tyr(3-I)-OH is responsible for catalyzing the first step of the noradrenergic biosynthesis pathway. H-Tyr(3-I)-OH is an effective tyrosine hydroxylase inhibitor.
S7483

DMOG

DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.
Cell Death Differ, 2020, 20
Cells, 2020, 9(3)
Int Immunopharmacol, 2020, 1;83:106438
S2173

Telotristat Etiprate (LX 1606 Hippurate)

Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Phase 3.
S2367

Tetrahydropapaverine HCl

Tetrahydropapaverine (Norlaudanosine), one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons.
Catalog No. Information Product Use Citations Product Validations
S1379

Isotretinoin

Isotretinoin (13-cis retinoic acid) was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.
Oncogene, 2020, 39(21):4212-4226
S9568

Sapropterin Dihydrochloride

Sapropterin Dihydrochloride, a synthetic preparation of the dihydrochloride salt of naturally occurring tetrahydrobiopterin (BH4), is a phenylalanine hydroxylase activator.
Tags: Hydroxylase activity | Dopamine-β-Hydroxylase activity | Hydroxylase inhibitor review