MedChemExpress LLC (MCE)

MedChemExpress - Model Bufexamac - 2438-72-4

Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug[1][2][3].

Bufexamac

MCE China：Bufexamac

Brand：MedChemExpress (MCE)

Cat. No.HY-B0494

CAS：2438-72-4

Synonyms：Bufexamic acid

Purity：98.0%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

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

Description：Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug.

In Vitro：Bufexamac (0.1-100 µM, 16 h) inhibits the secretion of IFN-α in peripheral blood mononuclear cells[1]. Bufexamac (30 µM, 6 days) inhibits HDAC10 to block autophagic flux in BE(2)-C cells and enhances the tumor-specific toxicity of DNA damage-inducing drugs[2]. Bufexamac (50-100 µM, 30 min) inhibits calcium ionophore A23187 stimulation of neutrophil chemotaxis via the inhibition of LTA4H-mediated endogenous LTB4 biosynthesis, with an IC50 of 12.91±4.02 μM for LTB4[3]. Bufexamac (0-500 µM, 4 h) inhibits lysine deacetylases (KDACs) at lower concentrations (>5 µM) and induces hypoxia-like responses in Hela cells by chelating cellular iron at higher concentrations (>200 µM) in Hela cells[4].

In Vivo：Bufexamac (50-100 mg/kg, p.o., seven days) ameliorates LPS-induced acute lung injury in mice by targeting LTA4H[3]. Bufexamac (20-100 mg, Intraarticular (IA) injection, weekly, 6 times) don’t cause any untoward systemic or local effects in healthy horse[5].

IC50 & Target：HDAC6 10.7 μM (Kd app) HDAC10 12.3 μM (Kd app) HDAC8 235 μM (Kd app) HDAC3 341 μM (Kd app)

References：

[1]. Bantscheff M, et al. Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes. Nat Biotechnol. 2011 Mar;29(3):255-65. [Content Brief]

[2]. Oehme I, et al. Histone deacetylase 10 promotes autophagy-mediated cell survival. Proc Natl Acad Sci U S A. 2013 Jul 9;110(28):E2592-601. [Content Brief]

[3]. Xiao Q, et al. Bufexamac ameliorates LPS-induced acute lung injury in mice by targeting LTA4H. Sci Rep. 2016 Apr 29;6:25298. [Content Brief]

[4]. Schölz C, et al. Acetylation site specificities of lysine deacetylase inhibitors in human cells. Nat Biotechnol. 2015 Apr;33(4):415-23. [Content Brief]

[5]. Suominen MM,et al. Effects of intra-articular injections of bufexamac suspension in healthy horses. Am J Vet Res. 2001 Oct;62(10):1629-35. [Content Brief]

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