HI TOPK 032

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Cat.No. 4555 - HI TOPK 032 | C20H11N5OS | CAS No. 487020-03-1
Description: Selective T-LAK-cell-originated protein kinase (TOPK) inhibitor
Chemical Name: N-(12-Cyanoindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

T-LAK-cell-originated protein kinase (TOPK) inhibitor; exhibits selectivity for TOPK over other MAPKK family members including ERK1, JNK1 and p38. Blocks proliferation of HCT116 colon cancer cells; suppresses tumor growth in a colon cancer xenograft model. Also inhibits Chk1 (IC50 = 9.6 μM).

Technical Data

M. Wt 369.4
Formula C20H11N5OS
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 487020-03-1
PubChem ID 1936439
InChI Key BCSBXWKRZUPFHW-UHFFFAOYSA-N
Smiles O=C(C5=CC=CS5)NC4=CC3=C(C#N)C2=NC1=CC=CC=C1N=C2N3C=C4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.39 20

Preparing Stock Solutions

The following data is based on the product molecular weight 369.4. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.71 mL 13.54 mL 27.07 mL
5 mM 0.54 mL 2.71 mL 5.41 mL
10 mM 0.27 mL 1.35 mL 2.71 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

Li et al (2011) Discovery of novel checkpoint kinase 1 inhibitors by virtual screening based on multiple crystal structures. J.Chem.Inf.Model. 51 2904 PMID: 21955044

Kim et al (2012) Novel TOPK inhibitor HI-TOPK-032 effectively suppresses colon cancer growth. Cancer Res. 72 3060 PMID: 22523035


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Citations for HI TOPK 032

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
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MAPK Signaling

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for HI TOPK 032

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