product name BG45
Description: BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 μM, 2.2 μM and >20 μM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively. BG45 selective for HDAC3 (IC50 = 289 nM) over HDAC1, 2. BG45 did not inihibit HDAC6 (IC50 >20 μM ). BG45 signigicantly inhibited tumor growth in a mouse model of multiple myeloma either alone and synergistically in combination with bortezomib. HDAC3 represents a promising therapeutic target, and validate a prototype novel HDAC3 inhibitor BG45 in MM.
References: Leukemia. 2014 Mar;28(3):680-9.
214.22
Formula
C11H10N4O
CAS No.
926259-99-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 42 mg/mL (196.1 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL warmed (9.3 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19424422
| In Vitro |
In vitro activity: BG45 causes significant cell growth inhibition and induces caspase-dependent apoptosis in a series of MM cells. In RPMI8226 cells, BG45 synergistically enhances bortezomib-induced cytotoxicity. Kinase Assay: Cell Assay: The growth inhibitory effects of BG45 in MM cell lines are assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT) dye absorbance. To measure proliferation of MM cells, the rate of DNA synthesis is measured by [3H]thymidine uptake. Cell lines: MM.1S, RPMI8226, U266, H929, MM.1 R, RPMI-LR5, OPM1, OPM2 and RPMI-DOX40 cells. |
|---|---|
| In Vivo | In mice bearing MM.1S xenograft of human MM, BG45 (50 mg/kg, i.p.) significantly inhibits MM tumor growth. When in combination with bortezomib, BG45 (50 mg/kg, i.p.) enhances bortezomib-induced cytotoxicity. |
| Animal model | Mice bearing MM.1S xenograft |
| Formulation & Dosage | Dissolved in 10% dimethylacetamide in 10% Kolliphor HS15 in PBS; 50 mg/kg, 5 days a week; i.p. injection |
| References | Leukemia. 2014 Mar;28(3):680-9. |
