BG45, HDAC3 Inhibitor

BG45 is a potent, selective and cell permeable HDAC3 inhibitor. It inhibits HDAC3 with IC50 of 289 nM. It has IC50 of 2.0 µM, 2.2 µM and >20 µM for HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively. BG45 triggers significant MM cell growth inhibition via apoptosis, evidenced by caspase and poly (ADP-ribose) polymerase cleavage. BG45 alone and in combination with bortezomib triggers significant tumor growth inhibition in vivo in a murine xenograft model of human MM.

Product information

CAS Number: 926259-99-6

Molecular Weight: 214.22

Formula: C11H10N4O

Chemical Name: N-(2-aminophenyl)pyrazine-2-carboxamide

Smiles: NC1=CC=CC=C1NC(=O)C1=CN=CC=N1

InChiKey: LMWPVSNHKACEKW-UHFFFAOYSA-N

InChi: InChI=1S/C11H10N4O/c12-8-3-1-2-4-9(8)15-11(16)10-7-13-5-6-14-10/h1-7H,12H2,(H,15,16)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

BG45 was used at 10 µM final concentration in various in vitro assays.

In Vivo:

BG45 was dosed to mice bearing MM.1S xenograft by IP injection at 50 mg/kg (5 days a week), significantly inhibits MM tumor growth. (Formulation: 10% dimethylacetamide in 10% Kolliphor HS15 in PBS)

References:

1. Minami J., et al. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. (2014) Leukemia. 28(3): 680-9.

Products are for research use only. Not for human use.

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