Art. -Nr.: HY-160426

Gcase activator 3

Name: Gcase activator 3
Brand: MedChemExpress
SKU: HY-160426
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Gcase activator 3 is a β-glucocerebrosidase (GCase) activator with an EC₅₀ of 1.49 μM. By binding to the allosteric site of GCase, Gcase activator 3 partially stabilizes GCase and enhances its activity. Gcase activator 3 can be conjugated with fluorophores to form fluorescent probes, which are used for high-throughput screening of GCase. Gcase activator 3 is applicable to research related to Gaucher's disease, Parkinson's disease, dementia with Lewy bodies, and multiple system atrophy.

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Reinheit: 99.67%
CAS. Nr.: 2270984-21-7
Formel: C₂₃H₂₀N₄O₂
Molecular Weight:384.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Gcase activator 3 Chemical Structure

CAS. Nr.: 2270984-21-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

β-glucocerebrosidase

1.49 μM (EC₅₀)

In Vitro

Gcase activator 3 (compound 9q) (48 nM-100 μM; 5 min pre-incubation, 30 min reaction incubation) activates recombinant wild-type β-glucocerebrosidase, with an AC₅₀ value of 1.49 μM and a maximum activity increase of up to 780%^[1].
Gcase activator 3 (5-15 μM; 3 days) increases the protein level of post-endoplasmic reticulum mature β-glucocerebrosidase in healthy control fibroblasts^[1].
Gcase activator 3 (5-15 μM; 3 days) increases the protein level of post-endoplasmic reticulum mature β-glucocerebrosidase in compound heterozygous GBA1^N370S/84GG mutant fibroblasts^[1].
Gcase activator 3 (5-15 μM; 3 days) dose-dependently increases lysosomal β-glucocerebrosidase activity in homozygous N370S and L444P GBA1 mutant fibroblasts^[1].
Gcase activator 3 (5-15 μM; 10 days) increases the protein level of post-endoplasmic reticulum mature β-glucocerebrosidase in dopamine neurons derived from wild-type control induced pluripotent stem cells (iPSCs)^[1].
Gcase activator 3 (5-15 μM; 10 days) increases the protein level of post-endoplasmic reticulum mature β-glucocerebrosidase in dopaminergic neurons differentiated from induced pluripotent stem cells (iPSC) derived from patients with heterozygous N370S GBA1 mutations^[1].

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

Western Blot Analysis^[1]

Cell Line:

Healthy control fibroblasts
Concentration:

5 μM; 15 μM
Incubation Time:

3 days
Result:

Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 1.4-fold relative to vehicle control at 15 μM.
Showed no significant change in activity relative to control at 5 μM.

Western Blot Analysis^[1]

Cell Line:

Compound heterozygous N370S/84GG GBA1 mutant fibroblasts
Concentration:

5 μM; 15 μM
Incubation Time:

3 days
Result:

Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 2.1-fold relative to vehicle control at 15 μM.
Showed no significant change in activity relative to control at 5 μM.

Western Blot Analysis^[1]

Cell Line:

Wild-type control induced pluripotent stem cell (iPSC)-derived dopaminergic neurons
Concentration:

5 μM; 15 μM
Incubation Time:

10 days
Result:

Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 1.3-fold relative to vehicle control at 15 μM.
Showed no significant change in activity relative to control at 5 μM.

Western Blot Analysis^[1]

Cell Line:

Heterozygous N370S GBA1 mutant iPSC-derived dopaminergic neurons
Concentration:

5 μM; 15 μM
Incubation Time:

10 days
Result:

Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 1.6-fold relative to vehicle control at 5 μM.
Increased post-ER (mature, lysosomal) GCase protein levels and enhanced GCase activity by 2.0-fold relative to vehicle control at 15 μM.

Chemical Information

CAS. Nr. 2270984-21-7
Appearance Solid
Molecular Weight 384.43
Formel C₂₃H₂₀N₄O₂
Color White to off-white
SMILES

CN(C[C@@H]1OC2=CC=CC=C2OC1)C3=C4C=CC=CC4=NC(C5=CC=CN=C5)=N3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (260.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6013 mL

13.0063 mL

26.0125 mL

5 mM

0.5203 mL

2.6013 mL

5.2025 mL

10 mM

0.2601 mL

1.3006 mL

2.6013 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (13.01 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zheng J, et al. Conversion of Quinazoline Modulators from Inhibitors to Activators of β-Glucocerebrosidase. Journal of medicinal chemistry. 2019 Feb 14;62(3):1218-1230. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6013 mL	13.0063 mL	26.0125 mL	65.0313 mL
	5 mM	0.5203 mL	2.6013 mL	5.2025 mL	13.0063 mL
	10 mM	0.2601 mL	1.3006 mL	2.6013 mL	6.5031 mL
	15 mM	0.1734 mL	0.8671 mL	1.7342 mL	4.3354 mL
	20 mM	0.1301 mL	0.6503 mL	1.3006 mL	3.2516 mL
	25 mM	0.1041 mL	0.5203 mL	1.0405 mL	2.6013 mL
	30 mM	0.0867 mL	0.4335 mL	0.8671 mL	2.1677 mL
	40 mM	0.0650 mL	0.3252 mL	0.6503 mL	1.6258 mL
	50 mM	0.0520 mL	0.2601 mL	0.5203 mL	1.3006 mL
	60 mM	0.0434 mL	0.2168 mL	0.4335 mL	1.0839 mL
	80 mM	0.0325 mL	0.1626 mL	0.3252 mL	0.8129 mL
	100 mM	0.0260 mL	0.1301 mL	0.2601 mL	0.6503 mL

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Gcase activator 3