Bezisterim

Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis[1][2][3]. Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[1001100-69-1]

Product Name Alternative

HE 3286; NE-3107

UNSPSC

12352211

Target

NF-κB

Type

Reference compound

Related Pathways

NF-κB

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/bezisterim.html

Purity

95.0

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O[C@@H]1[C@@]2([H])[C@@]3([H])[C@@]([C@@](C#C)(O)CC3)(CC[C@]2([H])[C@]4(C)C(C[C@@H](O)CC4)=C1)C

Molecular Formula

C21H30O3

Molecular Weight

330.46

References & Citations

[1]Auci D, et al. A new orally bioavailable synthetic androstene inhibits collagen-induced arthritis in the mouse: androstene hormones as regulators of regulatory T cells. Ann N Y Acad Sci. 2007;1110:630-640.|[2]Khan RS, et al. HE3286 reduces axonal loss and preserves retinal ganglion cell function in experimental optic neuritis. Invest Ophthalmol Vis Sci. 2014;55 (9) :5744-5751. Published 2014 Aug 19.|[3]Lu M, et al. A new antidiabetic compound attenuates inflammation and insulin resistance in Zucker diabetic fatty rats. Am J Physiol Endocrinol Metab. 2010;298 (5) :E1036-E1048.|[4]Nicoletti F, et al. 17α-Ethynyl-androst-5-ene-3β,7β,17β-triol (HE3286) Is Neuroprotective and Reduces Motor Impairment and Neuroinflammation in a Murine MPTP Model of Parkinson's Disease. Parkinsons Dis. 2012;2012:969418.