BG45

Catalog No.S7689 Batch:S768901

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Technical Data

Formula

C11H10N4O
Molecular Weight 214.22 CAS No. 926259-99-6
Solubility (25°C)* In vitro DMSO 42 mg/mL (196.06 mM)
Ethanol 2 mg/mL (9.33 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

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.
Targets
HDAC3 [1] HDAC1 [1] HDAC2 [1]
289 nM 2 μM 2.2 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]

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    MM.1S, RPMI8226, U266, H929, MM.1 R, RPMI-LR5, OPM1, OPM2 and RPMI-DOX40 cells

  • Concentrations

    ~30 μM

  • Incubation Time

    48 h

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Mice bearing MM.1S xenograft

  • Dosages

    50 mg/kg, 5 days a week

  • Administration

    i.p.

Selleck's BG45 has been cited by 6 publications

HDAC Inhibition Induces CD26 Expression on Multiple Myeloma Cells via the c-Myc/Sp1-mediated Promoter Activation [ Cancer Res Commun, 2024, 4(2):349-364] PubMed: 38284882
Selective Targeting of Class I HDAC Reduces Microglial Inflammation in the Entorhinal Cortex of Young APP/PS1 Mice [ Int J Mol Sci, 2023, 24(5)4805] PubMed: 36902234
A Class I HDAC Inhibitor BG45 Alleviates Cognitive Impairment through the CaMKII/ITPKA/Ca2+ Signaling Pathway [ Pharmaceuticals (Basel), 2022, 15(12)1481] PubMed: 36558932
HDAC8 cooperates with SMAD3/4 complex to suppress SIRT7 and promote cell survival and migration. [ Nucleic Acids Res, 2020, 6;48(6):2912-2923] PubMed: 31970414
Class I HDAC Inhibitor Improves Synaptic Proteins and Repairs Cytoskeleton Through Regulating Synapse-Related Genes In vitro and In vivo [ Front Aging Neurosci, 2020, 12:619866] PubMed: 33542682
Histone deacetylase inhibitor BG45-mediated HO-1 expression induces apoptosis of multiple myeloma cells by the JAK2/STAT3 pathway [ Anticancer Drugs, 2018, 29(1):61-74] PubMed: 29049036

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.