Art. -Nr.: HY-173366

dGEM3

Name: dGEM3
Brand: MedChemExpress
SKU: HY-173366
Price: 505.00 USD
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dGEM3 is a selective GEMIN3 Molecular glue degrader with a DC₅₀ of 680 nM. dGEM3 recruits GEMIN3 to the VHL E3 ligase, and mediates the targeted ubiquitination and degradation of GEMIN3 via the ubiquitin-proteasome system. dGEM3 induces extensive transcriptomic changes, including upregulation of ER stress response genes and downregulation of mRNA splicing genes. dGEM3 can be used in research related to amyotrophic lateral sclerosis, spinal muscular atrophy and neuromuscular dysfunction.

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Reinheit: 99.22%
Formel: C₃₁H₃₅Cl₂N₅O₅
Molecular Weight:628.55

Speicherung:

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

dGEM3 Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC50	870 nM	Displacement of VHL tracer in HEK293T cells transfected with NanoLuc-VHL incubated for 2 h by NanoBRET target engagement assay. Displacement of VHL tracer in HEK293T cells transfected with NanoLuc-VHL incubated for 2 h by NanoBRET target engagement assay.	2025.03.19.644003v1
HEK-293T	DC₅₀	680 nM	Degradation of endogenously tagged HiBiT-GEMIN3 in HEK293T cells incubated for 15 h following 1 h pre-treatment with ubiquitin-proteasome system inhibitors by HiBiT-GEMIN3 degradation assay. Degradation of endogenously tagged HiBiT-GEMIN3 in HEK293T cells incubated for 15 h following 1 h pre-treatment with ubiquitin-proteasome system inhibitors by HiBiT-GEMIN3 degradation assay.	2025.03.19.644003v1
HEK-293T	EC50	0.58 μM	Ternary complex formation between VHL-LgBiT and full-length SmBiT-GEMIN3 in HEK293T cells incubated for 2 h following 30-minute pre-treatment with 1 μM proteasome inhibitor by cellular NanoBiT ternary complex formation assay. Ternary complex formation between VHL-LgBiT and full-length SmBiT-GEMIN3 in HEK293T cells incubated for 2 h following 30-minute pre-treatment with 1 μM proteasome inhibitor by cellular NanoBiT ternary complex formation assay.	2025.03.19.644003v1
HEK-293T	EC50	560 nM	Ternary complex formation between VHL-LgBiT and SmBiT-GEMIN3 helicase domain (aa1-445) in HEK293T cells incubated for 2 h following 30-minute pre-treatment with 1 μM proteasome inhibitor by cellular NanoBiT ternary complex formation assay. Ternary complex formation between VHL-LgBiT and SmBiT-GEMIN3 helicase domain (aa1-445) in HEK293T cells incubated for 2 h following 30-minute pre-treatment with 1 μM proteasome inhibitor by cellular NanoBiT ternary complex formation assay.	2025.03.19.644003v1
HEK-293T	EC50	130 nM	Ternary complex formation between VHL-LgBiT and SmBiT-GEMIN3 ATP-binding domain (aa41-268) in HEK293T cells incubated for 2 h following 30-minute pre-treatment with 1 μM proteasome inhibitor by cellular NanoBiT ternary complex formation assay. Ternary complex formation between VHL-LgBiT and SmBiT-GEMIN3 ATP-binding domain (aa41-268) in HEK293T cells incubated for 2 h following 30-minute pre-treatment with 1 μM proteasome inhibitor by cellular NanoBiT ternary complex formation assay.	2025.03.19.644003v1
HEK-293T	EC50	5.72 μM	Ternary complex formation between VHL-LgBiT and full-length SmBiT-GEMIN3 in HEK293T cells incubated for 2 h following pre-treatment with 1 μM proteasome inhibitor and 10 μM VHL E3 ligase inhibitor by cellular NanoBiT ternary complex formation assay. Ternary complex formation between VHL-LgBiT and full-length SmBiT-GEMIN3 in HEK293T cells incubated for 2 h following pre-treatment with 1 μM proteasome inhibitor and 10 μM VHL E3 ligase inhibitor by cellular NanoBiT ternary complex formation assay.	2025.03.19.644003v1
HEK-293T	EC50	5.26 μM	Ternary complex formation between VHL-LgBiT and SmBiT-GEMIN3 helicase domain (aa1-445) in HEK293T cells incubated for 2 h following pre-treatment with 1 μM proteasome inhibitor and 10 μM VHL E3 ligase inhibitor by cellular NanoBiT ternary complex formation assay. Ternary complex formation between VHL-LgBiT and SmBiT-GEMIN3 helicase domain (aa1-445) in HEK293T cells incubated for 2 h following pre-treatment with 1 μM proteasome inhibitor and 10 μM VHL E3 ligase inhibitor by cellular NanoBiT ternary complex formation assay.	2025.03.19.644003v1
HEK-293T	EC50	1.10 μM	Ternary complex formation between VHL-LgBiT and SmBiT-GEMIN3 ATP-binding domain (aa41-268) in HEK293T cells incubated for 2 h following pre-treatment with 1 μM proteasome inhibitor and 10 μM VHL E3 ligase inhibitor by cellular NanoBiT ternary complex formation assay. Ternary complex formation between VHL-LgBiT and SmBiT-GEMIN3 ATP-binding domain (aa41-268) in HEK293T cells incubated for 2 h following pre-treatment with 1 μM proteasome inhibitor and 10 μM VHL E3 ligase inhibitor by cellular NanoBiT ternary complex formation assay.	2025.03.19.644003v1

In Vitro

dGEM3 (0.001-100 μM; 2 h) binds to VHL in HEK293T cells with an IC₅₀ of 870 nM^[1].
dGEM3 (10 μM) selectively degrades GEMIN3 in a VHL-dependent manner in HEK293T, MV-4-11, MCF-7, JVM-3, and SH-SY5Y cells, with no degradation observed in VHL-deficient 786-O cells^[1].
dGEM3 (0.01-10 μM; 6-18 h) degrades GEMIN3 in HiBiT-GEMIN3 HEK293T cells with a DC₅₀ of 680 nM, reaching 75% maximal degradation at 18 h, via a VHL- and ubiquitin-proteasome system-dependent mechanism^[1].
dGEM3 selectively degrades the helicase GEMIN3 by acting as a molecular glue that bridges the canonical VHL E3 ligase pocket and GEMIN3’s ATP-binding lobe to form a productive ternary complex^[2].
dGEM3 (10 μM; 6 h) alters the transcriptome of HEK293T cells, with changes in ER stress response and mRNA splicing pathways^[1].

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

Chemical Information

Appearance Solid
Molecular Weight 628.55
Formel C₃₁H₃₅Cl₂N₅O₅
Color White to off-white
SMILES

O=C(N[C@@H](C(C)(C)C)C(N1[C@H](C(NCC2=CC=C(C3=C(Cl)C=C(Cl)C=C3)C=C2)=O)C[C@@H](O)C1)=O)C4=C5N(N=C4)CCCO5
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 (159.10 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

1.5910 mL

7.9548 mL

15.9096 mL

5 mM

0.3182 mL

1.5910 mL

3.1819 mL

10 mM

0.1591 mL

0.7955 mL

1.5910 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Bushman J W, et al. Discovery of a VHL molecular glue degrader of GEMIN3 by Picowell RNA-seq[J]. bioRxiv, 2025: 2025.03. 19.644003.

[2]. Kozicka Z, et al. Clues for glues: from serendipity to nature's blueprints in degrader discovery. Essays in biochemistry. 2025 Dec 22;69(4):379-391.

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	1.5910 mL	7.9548 mL	15.9096 mL	39.7741 mL
	5 mM	0.3182 mL	1.5910 mL	3.1819 mL	7.9548 mL
	10 mM	0.1591 mL	0.7955 mL	1.5910 mL	3.9774 mL
	15 mM	0.1061 mL	0.5303 mL	1.0606 mL	2.6516 mL
	20 mM	0.0795 mL	0.3977 mL	0.7955 mL	1.9887 mL
	25 mM	0.0636 mL	0.3182 mL	0.6364 mL	1.5910 mL
	30 mM	0.0530 mL	0.2652 mL	0.5303 mL	1.3258 mL
	40 mM	0.0398 mL	0.1989 mL	0.3977 mL	0.9944 mL
	50 mM	0.0318 mL	0.1591 mL	0.3182 mL	0.7955 mL
	60 mM	0.0265 mL	0.1326 mL	0.2652 mL	0.6629 mL
	80 mM	0.0199 mL	0.0994 mL	0.1989 mL	0.4972 mL
	100 mM	0.0159 mL	0.0795 mL	0.1591 mL	0.3977 mL

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dGEM3

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dGEM3 Related Classifications

HY-173366 Related Classifications

Bioz