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BAU-243

Chemical Structure : BAU-243

CAS No.: 496767-27-2

BAU-243 (BAU243, AN-698/40780701)

Catalog No.: PC-20689Not For Human Use, Lab Use Only.

BAU-243 (BAU243) is a novel BH3 mimetic Bcl-2 inhibitor with a high affinity, effectively reduces overall GBM cell proliferation including a subpopulation of cancer-initiating cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BAU-243 (BAU243) is a novel BH3 mimetic Bcl-2 inhibitor with a high affinity, effectively reduces overall GBM cell proliferation including a subpopulation of cancer-initiating cells.
BAU-243 reduces survival of GBM cells and tumor-initiating stem cells (A172 cells, IC50=18.2 uM).
BAU-243 induces limited apoptosis and cell cycle arrest in low Bcl-2 expressing cells.
BAU-243 does not induce apoptosis in high Bcl-2 expressing SHSY-5Y cells despite the significant anti-proliferative effect.
BAU-243 promotes autophagic cell death through the disruption of Beclin 1 and Bcl-2 interaction, regardless of Bcl-2 expression level.
BAU-243 (25 mg/kg) reduced tumor growth in vivo with lower dose compared to other BH3 mimetics (ABT-263, 75 mg/kg).
BAU-243 demonstrated a remarkable anti-proliferative effect on the cancer sub-population that is considered a true representative of tumor-initiating GBM stem-like cells.
BAU-243 interacts with critical residues of Bcl-2 that plays role in the binding of Beclin 1 BH3 domain, showing that it can hinder Beclin 1:Bcl-2 complex formation, freeing Beclin 1 to activate the autophagy pathway.

Physicochemical Properties

M.Wt 501.60
Formula C28H27N3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(NC1=CC=C(C)C=C1)COC2=CC=C(/C=C(S/C(N3CCOC)=N\C4=CC=CC=C4)/C3=O)C=C2

References

1. Calis S, et al. Cell Death Discov. 2022 Oct 29;8(1):433.

2. Tutumlu G, et al. Front Chem. 2020;8.

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