dGEM3
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.22%
- 分子式: C31H35Cl2N5O5
- 分子量:628.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
870 nM
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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.
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2025.03.19.644003v1 |
| HEK-293T | DC50 |
680 nM
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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.
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2025.03.19.644003v1 |
| HEK-293T | EC50 |
0.58 μM
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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.
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2025.03.19.644003v1 |
| HEK-293T | EC50 |
560 nM
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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.
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2025.03.19.644003v1 |
| HEK-293T | EC50 |
130 nM
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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.
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2025.03.19.644003v1 |
| HEK-293T | EC50 |
5.72 μM
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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.
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2025.03.19.644003v1 |
| HEK-293T | EC50 |
5.26 μM
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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.
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2025.03.19.644003v1 |
| HEK-293T | EC50 |
1.10 μM
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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.
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2025.03.19.644003v1 |
体外実験
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.
化学情報
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性状 Solid
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分子量 628.55
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分子式 C31H35Cl2N5O5
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Color White to off-white
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (284 KB)
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SDS (252 KB)
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- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
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.
| 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 |
dGEM3 関連分類
HY-173366 関連分類
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