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BG45 Novel HDAC3-selective inhibitor

Catalog No.B5949
Size Price Stock Qty
5mg
$50.00
In stock
10mg
$75.00
In stock
50mg
$250.00
In stock
200mg
$490.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

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Chemical structure

BG45

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Chemical Properties

Cas No. 926259-99-6 SDF Download SDF
Chemical Name (Z)-N-(2-aminophenyl)pyrazine-2-carbimidic acid
Canonical SMILES NC1=CC=CC=C1/N=C(O)/C2=CN=CC=N2
Formula C11H10N4O M.Wt 214.22
Solubility Soluble in DMSO Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Description:

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.

Reference:
[1] Minami J, Suzuki R, Mazitschek R, Gorgun G, Ghosh B, Cirstea D, Hu Y, Mimura N, Ohguchi H, Cottini F, Jakubikova J, Munshi NC, Haggarty SJ, Richardson PG, Hideshima T, Anderson KC.  Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar;28(3):680-9.