Benserazide (hydrochloride)

Benserazide is a peripherally restricted inhibitor of aromatic L-amino acid decarboxylase (AADC, IC50 = 0.53 µM). It also inhibits tryptophan oxygenase and kynureninase (Kis = 41.8 and 26.4 µM, respectively, in rat liver homogenates), as well as hexokinase 2 (HK2), HK1, and HK4 (IC50s = 5.5, 25.1, and 40.5 µM, respectively, for the recombinant human enzymes). Benserazide (50-400 µM) is cytotoxic to SW480 colorectal cancer cells, an effect that can be reversed by HK2 siRNA knockdown, and inhibits proliferation of SW480, LoVo, HCT116, MCF-7, and SMMC-7721 cancer cells with IC50 values of 143, 151, 181.4, 186, and 210.4 nM, respectively. It reduces tumor growth in an SW480 mouse xenograft model when administered at doses of 300 and 600 mg/kg per day for 16 days. Benserazide (10 and 50 mg/kg) inhibits striatal AADC and enhances L-DOPA-induced increases in striatal dopamine levels in a mouse model of Parkinson's disease induced by 6-OHDA (Cay-25330).Formal Name: 2-[(2,3,4-trihydroxyphenyl)methyl]hydrazide-serine, monohydrochloride. CAS Number: 14919-77-8. Synonyms: Ro 4-4602. Molecular Formula: C10H15N3O5 . HCl. Formula Weight: 293.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/mL, DMSO: 16 mg/mL, PBS (pH 7.2): 5 mg/mL. lambdamax: 338 nm. SMILES: OC1=C(O)C=CC(CNNC(C(N)CO)=O)=C1O.Cl. InChi Code: InChI=1S/C10H15N3O5.ClH/c11-6(4-14)10(18)13-12-3-5-1-2-7(15)9(17)8(5)16,/h1-2,6,12,14-17H,3-4,11H2,(H,13,18),1H. InChi Key: ULFCBIUXQQYDEI-UHFFFAOYSA-N.