B-AP15

SKU: orb1307069

Description

B-AP15

Research Area

Cell Biology, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 1009817-63-3
• MW: 419.39
• Purity: 95.07%
• Formula: C₂₂H₁₇N₃O₆
• SMILES: C(=C\1/C(=O)\C(=C\C2=CC=C(N(=O)=O)C=C2)\CN(C(C=C)=O)C1)\C3=CC=C(N(=O)=O)C=C3
• Target: Apoptosis,DUB
• Solubility: DMSO:1 mg/mL (2.38 mM)

Bioactivity

• Target IC50:
  UCHL5:2.1 μM
• In Vivo:
  As a UPS (Ubiquitin-Proteasome System) inhibitor, B-AP15 induces cell death by triggerin the cathepsin-D-dependent lysosomal apoptotic pathway. Compared to peripheral blood mononuclear cells or immortalized epithelial cells (hTERT-RPE1), B-AP15 exhibits greater cytotoxicity towards HCT-116 cells. It dose-dependently accumulate the UbG76V-YFP receptor IC50 0.8 μM), indicating impaired proteasomal degradation. When applied to human colon cancer HCT-116 cells, B-AP15 (1 μM) rapidly accumulates polyubiquitinated proteins. At a concentration of 1 μM, B-AP15 inhibit the release of IL-1β induced by ATP from lipopolysaccharide-induced peritoneal macrophages. In THP-1 cells, 1 μM B-AP15 reduce the level of cell death induced by nigericin and significantly decrease the formation of ASC specks in lipopolysaccharide-induced THP-1 cells treated with nigericin. Additionally, B-AP15 (1 μM) causes a G2/M phase cell cycle arrest and accumulation of cell cycle inhibitors in HCT-116 cells. At 2.2 μM, B-AP15 dose-dependently increase the levels o the cyclin-dependent kinase inhibitors CDKN1A and CDKN1B, an the tumor suppressor gene TP53, without affectin the levels of ornithine decarboxylase 1.
• In Vitro:
  In mice with HCT-116 colon carcinoma xenografts, B-AP15 (5 mg/kg) significantly delayed tumor onset. Additionally, in severely immunodeficient mice bearing squamous cell carcinoma xenografts, B-AP15 (5 mg/kg) demonstrated notable antitumor activity.
• Cell Research:
  b-AP15 is dissolved in DMSO and stored, and then diluted with appropriate medium before us. Cell viability is monitored by eithe the fluorometric microculture cytotoxicity assay o the MTT assay. Fo the MTT assay, cells are seeded into 96-well flat-bottomed plates overnight and exposed to drugs, using DMSO a the control. A the end of incubations, 10 μL of a stock solution of 5 mg mL MTT is added into Each well, an the plates are incubated 4 hours at 37℃. Formazan crystals are dissolved with 100 μL 10% SDS/10 mM HCl solution overnight at 37℃. Absorbance is measured using an enzyme-linked immunosorbent assay (ELISA) plate reader at 590 n.

Storage & Handling

• Storage: Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

BAP15, B-AP15, b-AP15, B-AP-15, Apoptosis, B AP15, Deubiquitinase, DUBs, inhibit, Inhibitor, NSC687852, NSC-687852, NSC 687852, UCH-L5

Compound Identifiers

PubChem CID

5351435