EPZ033294
Based on 1 Customer Validation
EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T.
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- Purity: 98.41%
- CAS No.: 1887195-17-6
- 화학식: C20H22ClN7O
- 분자량:411.89
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
SYMD2 [1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KYSE-150 cell line | IC50 |
>40 nM
Compound: 9; EPZ033294
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Antiproliferative activity against human KYSE-150 cells assessed as inhibition of cell proliferation
Antiproliferative activity against human KYSE-150 cells assessed as inhibition of cell proliferation
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[PMID: 35914250] |
EPZ033294 (0-50 µM) has an inhibitory effect on SMYD2 and a concentration-dependent inhibitory effect in 293T [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:293T
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Concentration:0, 3.12, 6.25, 12.5, 25 and 50 µM
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Incubation Time:1000 s
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Result:Inhibited SMYD2.
Chemical Information
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CAS No. 1887195-17-6
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Appearance Solid
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분자량 411.89
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화학식 C20H22ClN7O
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Color White to light yellow
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SMILES
O=C(C1=CN(C2CC2)N=N1)NC3CN(C3)CC4=CN(CC5=CC=C(C=C5)Cl)N=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 25 mg/mL (60.70 mM; ultrasonic and warming and heat to 60°C; 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 (6.07 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 (6.07 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.
순도&문서
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Data Sheet (271 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Edoardo Fabini, et al. Small-molecule inhibitors of lysine methyltransferases SMYD2 and SMYD3: current trends. Medicinal Chemistry. 2019 Apr;11(8):901-921. [Content Brief]
[2]. Michael J, et al. Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation. PLOS ONE. 2018 Jun 1;13(6):e0197372. [Content Brief]
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 | 2.4278 mL | 12.1392 mL | 24.2783 mL | 60.6958 mL |
| 5 mM | 0.4856 mL | 2.4278 mL | 4.8557 mL | 12.1392 mL | |
| 10 mM | 0.2428 mL | 1.2139 mL | 2.4278 mL | 6.0696 mL | |
| 15 mM | 0.1619 mL | 0.8093 mL | 1.6186 mL | 4.0464 mL | |
| 20 mM | 0.1214 mL | 0.6070 mL | 1.2139 mL | 3.0348 mL | |
| 25 mM | 0.0971 mL | 0.4856 mL | 0.9711 mL | 2.4278 mL | |
| 30 mM | 0.0809 mL | 0.4046 mL | 0.8093 mL | 2.0232 mL | |
| 40 mM | 0.0607 mL | 0.3035 mL | 0.6070 mL | 1.5174 mL | |
| 50 mM | 0.0486 mL | 0.2428 mL | 0.4856 mL | 1.2139 mL | |
| 60 mM | 0.0405 mL | 0.2023 mL | 0.4046 mL | 1.0116 mL |
EPZ033294 Related Classifications
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