539187

Proteasome Inhibitor X, PI-083

The Proteasome Inhibitor X, PI-083, also referenced under CAS 6298-15-3, controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(e): Proteasome Inhibitor X, PI-083, NSC-45382
• Empirische Formel (Hill-System): C₂₁H₁₄ClN₃O₄S
• CAS-Nummer: 6298-15-3
• Molekulargewicht: 439.87
• UNSPSC Code: 12352200
• Assay: >95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Quality Segment: 100
• assay: >95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: dark red
• solubility: DMSO: 25 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C21H14ClN3O4S/c22-18-19(21(27)16-6-2-1-5-15(16)20(18)26)24-13-8-10-14(11-9-13)30(28,29)25-17-7-3-4-12-23-17/h1-12,24H,(H,23,25)
• InChI key: QRPKNPKHGNUFGK-UHFFFAOYSA-N

Beschreibung

General description

A cell-permeable, reversible 20S proteasome inhibitor with IC₅₀ values of 1 µM, 4.5 µM and 4.5 µM for CT-L, T-L and PGPH-L respectively. Exhibits CT-L (chymotrypsin-like) and cell proliferation inhibition selectively in ovarian, pancreatic, and breast cancer cells (T80-Hras, C7-Kras, and MCF-7, respectively) over their non-transformed counterparts (T80, C7, and MCF-10A), and induction of apoptosis with IC₅₀ values of 3.7 µM in an MTT assay on bone marrow cells isolated from multiple myeloma patients in vitro. Shown to have anti-tumor activities in a nude mouse xenograft model implanted with MCF-7 and A549 cells in vivo when dosed at 1 mpk, leading to significant tumor growth inhibition of 84%. PI-083 results in 43, 12 and 34% inhibition of tumor CT-L, T-L and PGPH activities respectively, compared to those of tumors from vehicle-treated controls, while it does not inhibit liver proteasome activities.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Lawrence, R., et al. 2010. Bioorg. Med. Chem.18, 5576.
Kazi, A., et al. 2009. Cell Cycle8, 1940.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 2