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614849 TOPK/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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide, TOPK Inhibitor, HI-TOPK-032, PBK Inhibitor, HI-TOPK-032

Primary Target: TOPK/PBK
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614849
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
487020-03-1C₂₀H₁₁N₅OS

Products

Catalog NumberPackaging Qty/Pack
614849-5MG Glass bottle 5 mg
Description
OverviewA 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.
Catalogue Number614849
Brand Family Calbiochem®
SynonymsN-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide, TOPK Inhibitor, HI-TOPK-032, PBK Inhibitor, HI-TOPK-032
References
ReferencesKim, D., et al. 2012, Cancer Res. 72, 3060.
Product Information
CAS number487020-03-1
FormRust solid
Hill FormulaC₂₀H₁₁N₅OS
Chemical formulaC₂₀H₁₁N₅OS
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetTOPK/PBK
Primary Target IC<sub>50</sub>2 µM
Purity≥ 98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-29°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
614849-5MG 04055977186338

Documentation

TOPK/PBK Inhibitor, HI-TOPK-032 - CAS 487020-03-1 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

TOPK/PBK Inhibitor, HI-TOPK-032 - CAS 487020-03-1 - Calbiochem Certificates of Analysis

TitleLot 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.

Revision27-June-2014 JSW
SynonymsN-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide, TOPK Inhibitor, HI-TOPK-032, PBK Inhibitor, HI-TOPK-032
DescriptionA 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.
FormRust solid
Intert gas (Yes/No) Packaged under inert gas
CAS number487020-03-1
Chemical formulaC₂₀H₁₁N₅OS
Purity≥ 98% by HPLC
SolubilityDMSO (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 InstructionsFollowing reconstitution, aliquot and freeze (-29°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesKim, D., et al. 2012, Cancer Res. 72, 3060.