CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC₅₀ of 0.9 μM for TAF1, and a K_d of 1.8 μM for TAF1 (2).

Kd: 1.8 μM (TAF1 (2))^[1]
IC50: 0.9 μM (TAF1)^[1]

CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC₅₀ of 0.9 μM for TAF1, and a K_d of 1.8 μM for TAF1 (2) and slso shows high affinity for the bromodomains of CREBBP, EP300, BRD9. CeMMEC1 (1, 10, 20 μM) decreases the number of THP1 cells in S phase in a dose manner. CeMMEC1 also induces apoptosis. CeMMEC1 in combination with (S)-JQ1 displays potently impaired cell viability than treatment alone^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

336.34

C₁₉H₁₆N₂O₄

440662-09-9

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 100 mg/mL (297.32 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.

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 (CeMMEC1) 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cells are seeded on clear flat-bottom 96-well or 384-well plates and treated with the indicated compounds (CeMMEC1) for the specified conditions. Live-cell imaging pictures are taken with the Operetta High Content Screening System, 20× objective and nonconfocal mode^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.