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MedChemExpress - Model EF24 - ...

MedChemExpress - Model EF24 - 342808-40-6

EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK[1][2][3][4].

EF24

MCE China：EF24

Brand：MedChemExpress (MCE)

Cat. No.HY-119272

CAS：342808-40-6

Purity：99.34%

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.

In Vitro：EF24 (0-10 μM) exhibits cytotoxicity against human breast cancer cells in a dose-dependent increase[2]. EF24 (0.1-100 μM, 6-72 h) effectively inhibits the active synthesis of DNA in both DU-145 prostate cancer cells and MDA-MB-231 breast cancer cells[3]. EF24 (20 μM, 24-72 h) induces cell cycle arrest and apoptosis by means of a redox-dependent mechanism and produces a time-dependent increase in intracellular ROS in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells[3].

In Vivo：EF24 (0.4 mg/kg, i.p., a single dose for 6 h) markedly ameliorates the post-hemorrhage morphologic changes and inflammatory cell infiltration, inhibits hemorrhage-induced NF-kB phosphorylation in rat model of hemorrhage[4].

References：

[1]. Lelli D, et al. Curcumin and treatment of melanoma: The potential role of microRNAs. Biomed Pharmacother. 2017 Apr;88:832-834. [Content Brief]

[2]. Mosley CA, et al. Highly active anticancer curcumin analogues. Adv Exp Med Biol. 2007;595:77-103. [Content Brief]

[3]. Adams BK, et al. EF24, a novel synthetic curcumin analog, induces apoptosis in cancer cells via a redox-dependent mechanism. Anticancer Drugs. 2005 Mar;16(3):263-75. [Content Brief]

[4]. Yadav VR, et al. Pharmacologic suppression of inflammation by a diphenyldifluoroketone, EF24, in a rat model of fixed-volume hemorrhage improves survival. J Pharmacol Exp Ther. 2013 Nov;347(2):346-56. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。