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(s):
TOPK/PBK Inhibitor, HI-TOPK-032
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About This Item
Empirical Formula (Hill Notation):
C20H11N5OS
CAS Number:
Molecular Weight:
369.40
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
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
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.
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
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)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
新产品
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 614849-5MG | 04055977186338 |