BG45 926259-99-6 GlpBio

www.glpbio.com

Product Data Sheet

Product Name: Cat. No.: Chemical Name:

BG45 GC12074

(Z)-N-(2-aminophenyl)pyrazine-2-carbimidic acid

CHEMICAL PROPERTIES Cas No.: 926259-99-6 Molecular Formula: Molecular Weight: Storage: Solubility:

Chemical Structure:

C11H10N4O 214.22 Powder

Soluble in DMSO

Background

IC50: 289 nM

Histone deacetylases (HDACs) represent novel molecular targets for the treatment of various types of cancers including multiple myeloma (MM). Many HDAC inhibitors have already shown remarkable anti-tumor activities in the preclinical studies, however, their clinical utility is limited due to unfavorable toxicities associated with their broad range HDAC inhibitory effects. BG45 is a novel small molecule HDAC3-selective inhibitor.

In vitro: BG45 is reported as an HDAC class I inhibitor with selectivity for HDAC3 over HDAC1, 2. Consistent with HDAC3 knockdown data, BG45 significantly inhibited MM cell growth dose-dependently. Importantly, BG45 also triggered a potent growth inhibitory effect against patient-derived MM cells, without affecting normal donor PBMCs [1].

In vivo: BG45 significantly inhibited MM tumor growth in a dose-dependent fashion. For example, significant differences were observed in control versus BG45 15 mg/kg, control versus BG45 50 mg/kg, and BG45 15 mg/kg versus BG45 50 mg/kg at day 22. Moreover, BG45 50 mg/kg in combination with bortezomib enhanced either single agent activity further. These results confirmed that BG45 triggers in vivo anti-MM activities [1].

Clinical trial: Up to now, BG45 is still in the preclinical development stage.

Research Update

1. Effect of Hydrofluoric Acid Concentration and Etching Time on Bond Strength to Lithium Disilicate Glass Ceramic. Oper Dent. 2017 Nov/Dec;42(6):606-615. doi: 10.2341/16-215-L. Epub 2017 Jul 14. PMID:28708007 Abstract

The aim of this study was to evaluate the influence of different concentrations of hydrofluoric acid (HF) associated with varied etching times on the microshear bond strength (μSBS) of a resin cement to a lithium disilicate glass ceramic. Two hundred seventy-five ceramic blocks (IPS e.max Press [EMX], Ivoclar Vivadent), measuring 8 mm × 3 mm thickness, were randomly distributed into five groups according to the HF concentrations (n=50): 1%, 2.5%, 5%, 7.5%, and 10%.

2. Does acid etching morphologically and chemically affect lithium disilicate glass ceramic surfaces? J Appl Biomater Funct Mater. 2017 Jan 26;15(1):e93-e100. doi: 10.5301/jabfm.5000303. PMID:27647389 Abstract

BACKGROUND: This study evaluated the surface morphology, chemical composition and adhesiveness of lithium disilicate glass ceramic after acid etching with hydrofluoric acid or phosphoric acid.METHODS: Lithium disilicate glass ceramic specimens polished by 600-grit silicon carbide paper were subjected to one or a combination of these surface treatments: airborne particle abrasion with 50-μm alumina (AA), etching with 5% hydrofluoric acid (HF) or 36% phosphoric acid (Phos), and application of silane coupling agent (Si). 3. Fatigue failure load of feldspathic ceramic crowns after hydrofluoric acid etching at different concentrations. J Prosthet Dent. 2018 Feb;119(2):278-285. doi: 10.1016/j.prosdent.2017.03.021. Epub 2017 May 26. PMID:28552291 Abstract

STATEMENT OF PROBLEM: Hydrofluoric acid etching modifies the cementation surface of ceramic restorations, which is the same surface where failure is initiated. Information regarding the influence of hydrofluoric acid etching on the cyclic loads to failure of ceramic crowns is lacking.PURPOSE: The purpose of this in vitro study was to evaluate the influence of different hydrofluoric acid concentrations on the fatigue failure loads of feldspathic ceramic crowns.