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614849
Sigma-AldrichTOPK/PBK Inhibitor, HI-TOPK-032 - CAS 487020-03-1 - Calbiochem
A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC₅₀ = 2 µM).
More>>A cell-permeable, selective, ATP competitive, reversible inhibitor of T-LAK-cell-originated protein kinase (IC₅₀ = 2 µM). Less<<
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Description
Overview
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.
TOPK/PBK Inhibitor, HI-TOPK-032 - CAS 487020-03-1 - Calbiochem Certificates of Analysis
Title
Lot Number
614849
References
Reference overview
Kim, D., et al. 2012, Cancer Res.72, 3060.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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.
Form
Rust solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
487020-03-1
Chemical formula
C₂₀H₁₁N₅OS
Purity
≥ 98% by HPLC
Solubility
DMSO (2.5 mg/ml). Use only fresh DMSO for reconstitution.
Storage
Protect from light +2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-29°C). Stock solutions are stable for up to 3 months at -20°C.