UNC10013
Based on 1 Customer Validation
UNC10013 is an inhibitor targeting the triple Tudor domain (3TD) of SETDB1. UNC10013 covalently binds to Cys385 of SETDB1 3TD, acts as a negative allosteric modulator of the methyltransferase domain of SETDB1, reduces the level of Akt methylation mediated by SETDB1, and blocks Tyr308 phosphorylation of Akt. UNC10013 is applicable to cancer-related research.
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- Purity: 99.90%
- 화학식: C37H54F12N8O9
- 분자량:982.85
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
More
Biological Activity
UNC10013 (0.057 μM; 1 h) potently displaces the H3K9Me2K14Ac peptide from wild-type SETDB1 3TD with an IC50 of 0.057 μM[1].
UNC10013 (8.2 μM; 1 h) has reduced potency displacing the H3K9Me2K14Ac peptide from SETDB1 3TDC385A, with an IC50 of 8.2 μM[1].
UNC10013 (12.5-200 nM; 20 min) shows potent targeted covalent reactivity toward SETDB1 3TD, with a kinact/KI ratio of 1.04 × 106 M-1 s-1, a kinact of 6.22 × 10-2 s-1, and a KI of 60 nM[1].
UNC10013 (0.07 μM; 1 h pre-incubation at room temperature) potently displaces the FITC-H3K9Me2K14Ac peptide from SETDB1 3TD with an IC50 of 0.07 μM[1].
UNC10013 (0.027 μM; 1 h) potently displaces the H3K9Me2K14Ac-modified nucleosome from SETDB1 3TD with an IC50 of 0.027 μM[1].
UNC10013 (dose-response curve concentrations) inhibits SETD2 and PRMT1 methyltransferase activities with IC50 values of 0.8 ± 0.1 μM and 1.3 ± 0.1 μM, respectively[1].
UNC10013 (10 μM; 1 h) shows high proteome-wide selectivity, covalently modifying only SETDB1 Cys385 and NCK2 Cys144 when incubated with MCF-7 cell lysate[1].
UNC10013 (10-40 μM; 24 h pretreatment) acts as a negative allosteric modulator of SETDB1, inhibiting SETDB1-mediated Akt methylation and subsequent Akt Tyr308 phosphorylation in HeLa cells at concentrations of 30 μM and above[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Oil
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분자량 982.85
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화학식 C37H54F12N8O9
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Color Colorless to light yellow
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SMILES
O=C(NC1=CC2=C(NCCCCCCN(C)C)N=C(NCCCCCN(C)C)N=C2C=C1)/C=C/CN(C)C.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 100 mg/mL (101.74 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.54 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (275 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
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 (sealed storage, away from moisture). 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 | 1.0174 mL | 5.0872 mL | 10.1745 mL | 25.4362 mL |
| 5 mM | 0.2035 mL | 1.0174 mL | 2.0349 mL | 5.0872 mL | |
| 10 mM | 0.1017 mL | 0.5087 mL | 1.0174 mL | 2.5436 mL | |
| 15 mM | 0.0678 mL | 0.3391 mL | 0.6783 mL | 1.6957 mL | |
| 20 mM | 0.0509 mL | 0.2544 mL | 0.5087 mL | 1.2718 mL | |
| 25 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0174 mL | |
| 30 mM | 0.0339 mL | 0.1696 mL | 0.3391 mL | 0.8479 mL | |
| 40 mM | 0.0254 mL | 0.1272 mL | 0.2544 mL | 0.6359 mL | |
| 50 mM | 0.0203 mL | 0.1017 mL | 0.2035 mL | 0.5087 mL | |
| 60 mM | 0.0170 mL | 0.0848 mL | 0.1696 mL | 0.4239 mL | |
| 80 mM | 0.0127 mL | 0.0636 mL | 0.1272 mL | 0.3180 mL | |
| 100 mM | 0.0102 mL | 0.0509 mL | 0.1017 mL | 0.2544 mL |
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