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BG45 is an HDAC I type inhibitor with IC50 of 289 nM, 2.0 μM, 2.2 μM and >20 μM for HDAC3/1/2/6 in cell-free assays, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $34 | In Stock | |
10 mg | $58 | In Stock | |
25 mg | $106 | In Stock | |
50 mg | $178 | In Stock | |
100 mg | $286 | In Stock | |
200 mg | $367 | In Stock | |
1 mL x 10 mM (in DMSO) | $38 | In Stock |
Description | BG45 is an HDAC I type inhibitor with IC50 of 289 nM, 2.0 μM, 2.2 μM and >20 μM for HDAC3/1/2/6 in cell-free assays, respectively. |
Targets&IC50 | HDAC3:289 nM, HDAC2:2.2 μM, HDAC1:2 μM |
In vitro | 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. [1] |
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. [1] |
Kinase Assay | Kinase assays: Initial rate constants are measured at 21 °C in the presence of 100 mM HEPES (pH 7.5), 0.3 mg/mL poly(Glu-Tyr) peptide substrate, 10 mM MgCl2, 1 mg/mL bovine serum albumin, 5% DMSO, 20 nM MET-KD and various concentrations of ATP and SGX523. Total reaction volumes (20 μL) are quenched with 20 μL Kinase-Glo detection buffer. Luminescence is detected in a plate-reading luminometer and the results are analyzed by nonlinear regression. |
Cell Research | 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.(Only for Reference) |
Molecular Weight | 214.22 |
Formula | C11H10N4O |
Cas No. | 926259-99-6 |
Smiles | Nc1ccccc1NC(=O)c1cnccn1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 2 mg/mL (9.33 mM), Heating is recommended. DMSO: 39 mg/mL (182.1 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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