PROTAC NSD3 degrader-1
Based on 1 Customer Validation
PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
(Pink: NSD3 ligand (HY-114208); Blue: VHL ligand (HY-112078); Black: linker (HY-W014831)).
For research use only. We do not sell to patients.
- Purity: 99.40%
- CAS No.: 3033543-95-9
- Formula: C56H71FN8O4S
- Molecular Weight:971.28
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
5.49 μM
Compound: 8; SYL2158
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Antiproliferative activity against human A549 cells incubated for 3 days by CCK-8 method
Antiproliferative activity against human A549 cells incubated for 3 days by CCK-8 method
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[PMID: 35717870] |
| NCI-H1703 | IC50 |
2.74 μM
Compound: 8; SYL2158
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Antiproliferative activity against human NCI-H1703 cells incubated for 6 days by CCK-8 method
Antiproliferative activity against human NCI-H1703 cells incubated for 6 days by CCK-8 method
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[PMID: 35717870] |
Chemical Information
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CAS No. 3033543-95-9
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Appearance Solid
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Molecular Weight 971.28
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Formula C56H71FN8O4S
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Color White to yellow
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SMILES
CC1=C(C(C)=CC(CNCCCCCCCCCCC(N[C@H](C(N2[C@@H](C[C@H](C2)O)C(N[C@H](C3=CC=C(C=C3)C4=C(N=CS4)C)C)=O)=O)C(C)(C)C)=O)=C1)C5=C(N(C=N5)C)C6=CC=NC7=C6C=CC(F)=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (102.96 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (2.57 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 (2.57 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.
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.
Purity & Documentation
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Data Sheet (272 KB)
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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)
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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 1.0296 mL | 5.1478 mL | 10.2957 mL | 25.7392 mL |
| 5 mM | 0.2059 mL | 1.0296 mL | 2.0591 mL | 5.1478 mL | |
| 10 mM | 0.1030 mL | 0.5148 mL | 1.0296 mL | 2.5739 mL | |
| 15 mM | 0.0686 mL | 0.3432 mL | 0.6864 mL | 1.7159 mL | |
| 20 mM | 0.0515 mL | 0.2574 mL | 0.5148 mL | 1.2870 mL | |
| 25 mM | 0.0412 mL | 0.2059 mL | 0.4118 mL | 1.0296 mL | |
| 30 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8580 mL | |
| 40 mM | 0.0257 mL | 0.1287 mL | 0.2574 mL | 0.6435 mL | |
| 50 mM | 0.0206 mL | 0.1030 mL | 0.2059 mL | 0.5148 mL | |
| 60 mM | 0.0172 mL | 0.0858 mL | 0.1716 mL | 0.4290 mL | |
| 80 mM | 0.0129 mL | 0.0643 mL | 0.1287 mL | 0.3217 mL | |
| 100 mM | 0.0103 mL | 0.0515 mL | 0.1030 mL | 0.2574 mL |
PROTAC NSD3 degrader-1 Related Classifications
HY-155816 Related Classifications
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