Glycosidase Modulator

NCGC 607 is a noninhibitory small-molecule chaperone of glucocerebrosidase (GCase). NCGC 607 can increase GCase activity, reduce α-synuclein levels, and decrease glycolipid levels. NCGC 607 can be used in the research of Gaucher disease and Parkinson's disease.

β-Glucocerebrosidase modulator 1 (Compound 28) is an allosteric modulator for β-Glucocerebrosidase with an EC₅₀ of 9.0 μM and a K_d of 0.050 μM.

ML198 is a glucocerebrosidase (GCase) modulator with an EC₅₀ of 0.4 μM. ML198 is an activator and non-inhibitory chaperone of glucocerebrosidase. ML198 can be used for the research of Gaucher disease. ML198 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

GCase modulator-1 (compound 9g), a derivative of Quinazoline, is a modulator of GCase (Glucosidase) (AC₅₀=2.23 μM).

OMJ-4 is a mutant alpha-mannosidase modulator. OMJ-4 can restore mutant alpha-mannosidase's catalytic function, and induces changes in compactness and active-site flexibility to improve substrate accommodation. OMJ-4 acts as an inducer of substrate reactivity, increasing the reactivity of mannose disaccharide bound to mutant alpha-mannosidase. OMJ-4 reduces the activation energy required for the enzymatic reaction of mutant alpha-mannosidase. OMJ-4 can be used for the research of alpha-mannosidosis.

G721-0377 is a CHI3L1 modulator with a human K_d value of 45 μM. G721-0377 binds to CHI3L1 and modulates downstream signaling pathways. G721-0377 suppresses CHI3L1-induced NF-κB activation, decreases secretion of CHI3L1 and IL-6. G721-0377 can be used for the research of Alzheimer's disease.

JZ-4109 is a β-Glucocerebrosidase (GCase) modulator with an IC₅₀ of 8 nM for wild-type recombinant GCase. JZ-4109 binds to an allosteric site at the GCase dimer interface, stabilizes wild-type and GCase^N370S mutant GCase, induces GCase dimerization. JZ-4109 increases GCase protein abundance. JZ-4109 can be used for the research of Parkinson's diseas.