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CeMMEC13

Catalog No.GC19099

CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 uM.

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CeMMEC13 Chemical Structure

Cas No.: 1790895-25-8

Size Price Stock Qty
5mg
$74.00
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10mg
$114.00
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25mg
$241.00
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50mg
$422.00
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100mg
$736.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of CeMMEC13

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.

Protocol of CeMMEC13

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.

Chemical Properties of CeMMEC13

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CeMMEC13

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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
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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. )

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Average Rating: 5 ★★★★★ (Based on Reviews and 16 reference(s) in Google Scholar.)

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