Bromosporine

SKU: orb1222635

Description

Bromosporine is a broad spectrum inhibitor for bromodomains and as such will be very useful in elucidating further biological roles of reader domains as well as a tool for the validation of functional assays. Proteins that contain BRDs have been implicated in the development of a large variety of diseases, including various cancers, inflammatory diseases and neurological diseases and the therapeutic potential of bromodomain inhibition has been shown in several of these diseases, such as HIV, cancer and inflammation.

Key Properties

• CAS Number: 1619994-69-2
• MW: 404.45
• Purity: >98% (HPLC)
• Formula: C₁₇H₂₀N₆O₄S
• SMILES: CCOC(=O)Nc1cc(nn2c(C)nnc12)c1cc(NS(=O)(=O)C)c(C)cc1
• Target: BRD
• Solubility: DMSO : ≥ 51.7 mg/mL; 127.83 mM

Bioactivity

• In Vivo:
  Animal model: Female BALB/c nude mice (5-6 weeks; injected with 1 × 106 cells/100 μL of HT116 cells). Dosage: 100 mg/kg. Administration: i.p.; daily for 10 days. Result: Exhibited better antitumor activity than individual Bromosporine or 5-FU (HY-90006) when co-treated with the two agent.
  Read more...
• In Vitro:
  Cell Proliferation Assay Cell line: HCT116 and HT29. Concentration: 0, 30, 60, 120, 240, 480 and 1000 nM. Incubation time: 72 h. Result: Synergistically inhibited cell growth in CRC cells with 5-FU (HY-90006) (0-16 μg/mL) and exhibited a dose-dependent manner. Cell Cycle Analysis Cell line: HCT116 and HT29. Concentration: Various concentration. Incubation time: 48 h. Result: Caused a distinct increase in the cells arrested at G1 phase when combined with 5-FU (HY-90006). Western blot analysis. Cell line: HCT116 and HT29. Concentration: Various concentration. Incubation time: 48 h. Result: Elevated the level of apoptosis in both cell lines through cleavage of PARP, caspase 3, and 9.Cell Proliferation Assay Cell line: MV4; 11, KASUMI-1, OCI-AML3 and K562. Concentration: 0.1, 0.5 and 1 μM Incubation time: 6-10 days. Result: Inhibited these AML cells in a dose-dependent manner. Cell Cytotoxicity Assay Cell line: PBMCs. Concentration: 1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM and 50 μM Incubation time: 48 h. Result: Did not induce marked toxicity in primary CD4+ T cells with CC50 over 10 μM.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bromosporine

Quick Database Links

Gene Symbol

BRD