CeMMEC13 |
| Catalog No.GC19099 |
CeMMEC13 es un potente inhibidor del bromodominio TAF1 (2), con una IC50 de 2,1 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1790895-25-8
Sample solution is provided at 25 µL, 10mM.
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CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 uM.
CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 uM. CeMMEC13 shows little or no effects on REDNESS, BRD4, CREBBP. CeMMEC13 (0-20 uM) in combination with (S)-JQ1 increases RFP expression in REDS3 cells and is effective reducing the viability of H23 and THP1 cells, better than that of single treatment[1].
References:
[1]. Sdelci S, et al. Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk. Nat Chem Biol. 2016 Jul;12(7):504-10.
Kinase experiment: | TAF1 binding assays are conducted using the EPIgeneous Binding Domain kit B. Binding is determined by the displacement of an acetylated biotin peptide from a GST-tagged TAF1 protein using HTRF with a Eu3+-conjugated GST antibody donor and streptavidin-conjugated acceptor. Compounds (CeMMEC13) are dispensed into assay plates, ProxiPlate-384 Plus using an Echo 525 Liquid Handler. Binding assays are conducted in a final volume of 20 μL with 5 nM TAF1-GST, 50 nM peptide (SGRGK (ac)GGK (ac)GLGK (ac)GGAK (ac)RHRK (biotin)-acid), 6.25 nM Streptavidin-XL665, 1:200 Anti-GST-Eu3+ cryptate and 0.1% DMSO. Assay reagents are dispensed into plates using a Multidrop combi and incubated at room temperature for 3 h. Fluorescence is measured using a PHERAstar microplate reader using the HTRF module with dual emission protocol (A = excitation of 320 nm, emmission of 665 nm, and B = excitation of 320 nm, emission of 620 nm). Raw data are processed to give an HTRF ratio (channel A/B × 10,000), which is used to generate IC50 curves[1]. |
Cell experiment: | Cells are seeded on clear flat-bottom 96-well or 384-well plates and treated with the indicated compounds (CeMMEC13) for the specified conditions. Live-cell imaging pictures are taken with the Operetta High Content Screening System, 20× objective and nonconfocal mode[1]. |
References: [1]. Sdelci S, et al. Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk. Nat Chem Biol. 2016 Jul;12(7):504-10. | |
| Cas No. | 1790895-25-8 | SDF | |
| Canonical SMILES | O=C(C1=CC(N(C)C2=C1C=CC=C2)=O)NC3=CC=C(OCCO4)C4=C3 | ||
| Formula | C19H16N2O4 | M.Wt | 336.34 |
| Solubility | DMSO : ≥ 30 mg/mL (89.20 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9732 mL | 14.8659 mL | 29.7318 mL |
| 5 mM | 0.5946 mL | 2.9732 mL | 5.9464 mL |
| 10 mM | 0.2973 mL | 1.4866 mL | 2.9732 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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