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MedChemExpress - Model Clofazimine - ...

MedChemExpress - Model Clofazimine - 2030-63-9

Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research[1][2][3][4][5].

Clofazimine

MCE China：Clofazimine

Brand：MedChemExpress (MCE)

Cat. No.HY-B1046

CAS：2030-63-9

Purity：99.79%

Storage：4°C, protect from light *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

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

Description：Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research.

In Vitro：Clofazimine (0.0625-2 mg/L, 14 d) exerts no apparent activity against M. tuberculosis during the first 2–4 days of exposure, exhibits a concentration-dependent antimicrobial activity after 1 week: bacteriostatic activity at concentrations at or below the 0.25 mg/L MIC and bactericidal activity at concentrations above the MIC. INH is used as positive control.[3]. Clofazimine (10 μM, 24 h) inhibits the growth of hematological cancer cell lines (Jurkat, U266, Namalwa, K562, HL60). For U266, Clofazimine (1-50 μM, 12-48 h) shows a dose- and time-dependent inhibitory effect[4]. Clofazimine (10 μM, 24-48 h) depolarizes the mitochondrial membrane, significantly increases active caspase-3 level (25-fold) and increases the percentage of early and late apoptotic cells in U266[4].

In Vivo：Clofazimine (100,50 mg/kg, p.o., once per day for 14 d) exhibits a delayed antimicrobial activity against Mycobacterium tuberculosis in mice[3].

IC50 & Target：Quinolone

References：

[1]. Riccardi N, et al. Clofazimine: an old drug for never-ending diseases. Future Microbiol. 2020，15:557-566. [Content Brief]

[2]. Arbiser JL, et al. Clofazimine: a review of its medical uses and mechanisms of action. J Am Acad Dermatol. 1995 Feb;32(2 Pt 1):241-7. [Content Brief]

[3]. Ammerman NC, et al. Clofazimine has delayed antimicrobial activity against Mycobacterium tuberculosis both in vitro and in vivo. J Antimicrob Chemother. 2017，72(2):455-461. [Content Brief]

[4]. Durusu İZ, et al. Anti-cancer effect of clofazimine as a single agent and in combination with cisplatin on U266 multiple myeloma cell line. Leuk Res. 2017，55:33-40. [Content Brief]

[5]. Ren YR, et al. Clofazimine Inhibits Human Kv1.3 Potassium Channel by Perturbing Calcium Oscillation in T Lymphocytes. PLoS One. 2008，3(12):e4009. [Content Brief]

[6]. Cholo MC, et al. Clofazimine: current status and future prospects. J Antimicrob Chemother. 2012 Feb;67(2):290-8. [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。