2. Metabolic Enzyme/Protease
  3. Glycosidase
  4. JZ-4109

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 GCaseN370S mutant GCase, induces GCase dimerization. JZ-4109 increases GCase protein abundance. JZ-4109 can be used for the research of Parkinson's diseas.

For research use only. We do not sell to patients.

JZ-4109

JZ-4109 Chemical Structure

CAS No. : 1997359-63-3

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JZ-4109 Related Antibodies

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Description

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 GCaseN370S mutant GCase, induces GCase dimerization. JZ-4109 increases GCase protein abundance. JZ-4109 can be used for the research of Parkinson's diseas[1].

In Vitro

JZ-4109 (Compound 3) (0.76 nM-1.56 μM;30 min) potently inhibits wild-type recombinant GCase with an IC50 of 8 nM via linear mixed inhibition[1].
JZ-4109 (0.25-100 μM; heated from 20 °C to 95 °C at 0.1 °C/s) stabilizes wild-type recombinant GCase against thermal denaturation[1].
JZ-4109 (0.2-2 μM; 3 days) significantly increases GCase protein abundance and enzyme activity in healthy control human fibroblast cells without altering GBA mRNA levels[1].
JZ-4109 (2 μM; 3 days) promotes maturation and trafficking of GCase to post-ER compartments in healthy control human fibroblast cells without increasing ER-retained GCase[1].
JZ-4109 (2 μM; 3 days) significantly increases GCase abundance and enzyme activity in lysosomal fractions of HEK cells[1].
JZ-4109 (0.2-2 μM; 3 days) significantly increases mature post-ER GCase protein abundance and enzyme activity in homozygous GBAN370S mutant human fibroblast cells from a type-1 Gaucher’s disease donor[1].
JZ-4109 (4.12-33.0 μM, co-incubated with 16.5 μM GCase) induces dose-dependent dimerization of wild-type GCase in solution[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JZ-4109 Related Antibodies

Western Blot Analysis[1]

Cell Line: Healthy control human fibroblast cells
Concentration: 0.2 μM; 2 μM
Incubation Time: 3 days
Result: Significantly increased GCase protein abundance relative to DMSO control at 0.2 μM.
Produced a greater significant increase in GCase protein abundance relative to DMSO control at 2 μM.
Significantly increased GCase enzyme activity relative to DMSO control at both 0.2 μM and 2 μM.

Western Blot Analysis[1]

Cell Line: HEK cells
Concentration: 2 μM
Incubation Time: 3 days
Result: Significantly increased GCase levels and enzyme activity in lysosomal enrichment fractions relative to DMSO control.
Showed a significant increase in GCase relative to lysosome marker Lamp1 relative to DMSO control.

Western Blot Analysis[1]

Cell Line: Homozygous N370S mutant human fibroblast cells (type-1 Gaucher’s disease patient)
Concentration: 0.2 μM; 2 μM
Incubation Time: 3 days
Result: Significantly increased GCase protein abundance and enzyme activity relative to DMSO control at 0.2 μM.
Produced a greater significant increase in GCase protein abundance and enzyme activity relative to DMSO control at 2 μM.
Localized the increase in GCase signal to post-ER mature GCase.
Molecular Weight

338.41

Formula

C22H18N4
CAS No.
SMILES

N1=CC=CC(=C1)C2=NC=3C=CC=CC3C(=N2)NC4CC=5C=CC=CC5C4
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JZ-4109 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JZ-41091997359-63-3JZ4109JZ 4109GlycosidaseHEK cellsN370S mutant GCaseER stressβ-GlucocerebrosidaseGCaselysosomesGBA mRNAfibroblast cellsParkinson's diseaseGaucher’s diseaseInhibitorinhibitorinhibit

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