614849

TOPK/PBK Inhibitor, HI-TOPK-032

A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC₅₀ = 2 µM).

• Synonym(e): TOPK/PBK Inhibitor, HI-TOPK-032
• Empirische Formel (Hill-System): C₂₀H₁₁N₅OS
• CAS-Nummer: 487020-03-1
• Molekulargewicht: 369.40
• MDL number: MFCD03286313
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• potency: 2 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: rust
• solubility: DMSO: 2.5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [s]1c(ccc1)C(=O)Nc2cc3[n](c4nc5c(nc4c3C#N)cccc5)cc2
• InChI: 1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26)
• InChI key: BCSBXWKRZUPFHW-UHFFFAOYSA-N

Beschreibung

General description

A cell-permeable, ATP competitive, reversible indolizinoquinoxalin derivative that acts as a specific inhibitor of T-LAK-cell-originated protein kinase (TOPK/PBK)(IC₅₀ = 2 µM). Does not affect the activities of ERK1, JNK1, and p38 MAP kinases. At higher concentrations (~ 5 µM) also inhibits MEK1 activity. Shown to suppress the proliferation of HCT116 colon cancer cell line and block tumor growth in colon cancer xenograft models in a dose-dependent manner. Diminishes TOPK activity only in cells over-expressing TOPK without significantly affecting cells with low levels of expression. Also shown to increase the expression of p53, active caspase-7, cleaved poly-ADP-Ribose polymerase, and increase the phosphorylation of Cdc2.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC₅₀ = 2 µM).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
TOPK/PBK

Preparation Note

Following reconstitution, aliquot and freeze (-29°C). Stock solutions are stable for up to 3 months at -20°C.

Use only fresh DMSO for reconstitution.

Other Notes

Kim, D., et al. 2012, Cancer Res.72, 3060.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable