GBA2-IN-2
GBA2-IN-2 is a brain-penetrant and selective GBA2 inhibitor (human IC50 = 319 nM; Ki = 2.1 μM). GBA2-IN-2 reacts covalently and irreversibly with the catalytic nucleophilic glutamate in the GBA2 active site. GBA2-IN-2 produces dose-dependent GBA2 inhibition in the brain, liver, kidney, and spleen of mice after intravenous administration, with no significant inhibition of GBA1 or GCS. GBA2-IN-2 can be used for research related to neurological lysosomal storage disorders and can also serve as a precursor for lead compound-related research.
For research use only. We do not sell to patients.
- Formula: C16H27NO3
- Molecular Weight:281.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
36 nM
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In-cellulo inhibition of GBA2 in living GBA2/GBA3-overexpressing HEK293T cells incubated 3 hrs with compound and labeled by ABP 23, assessed by SDS-PAGE fluorescence quantification.
In-cellulo inhibition of GBA2 in living GBA2/GBA3-overexpressing HEK293T cells incubated 3 hrs with compound and labeled by ABP 23, assessed by SDS-PAGE fluorescence quantification.
|
42913544 |
In Vitro
GBA2-IN-2 (0-100,000 nM) inhibits GBA2 in HEK293T lysates with an apparent cABPP IC50 of 184 nM, while it does not inhibit GBA1 or GBA3 at concentrations up to 100,000 nM[1].
GBA2-IN-2 covalently inactivates GBA2 with a Ki of 2.1 µM and a kinact of 1.42 min-1, corresponding to a kinact/Ki of 663 min-1 mM-1[1].
GBA2-IN-2 (0-50,000 nM; 3 h) inhibits GBA2 with an in cellulo IC50 of 36 nM in live HEK293T cells overexpressing GBA2/GBA3, and does not affect GBA1 and GBA3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 281.39
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Formula C16H27NO3
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SMILES
O[C@H]1[C@H](O)[C@@H](CO)[C@@H]2[C@H]1N2CCCCCCCCC#C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GBA2-IN-2 Related Classifications
HY-190905 Related Classifications
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