Hydroxylase

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.

S4586New

4-Chloro-DL-phenylalanine

4-Chloro-DL-phenylalanine 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.

S7456New

LCI699

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

S8172New

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.

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.

S7483

DMOG

DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolyl hydroxylase.

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

S1379

Isotretinoin

It was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.

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.

S4586New

4-Chloro-DL-phenylalanine

4-Chloro-DL-phenylalanine 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.

S7456New

LCI699

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

S8172New

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.

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.

S7483

DMOG

DMOG is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolyl hydroxylase.

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, 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

It was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.

Tags: Hydroxylase activity | Dopamine-β-Hydroxylase activity | Hydroxylase inhibitor review