Abstract

This article contains chemical characterization and biological activity data for a novel indirubin derivative, termed LDD-1819. The detailed synthesis procedure and associated NMR data are presented. The concentration-dependent inhibition data of two biological targets, glycogen synthase kinase-3β and aurora kinase A are described. The following biological data are also contained in this article: 1) the cellularization of skeletal muscle myotubes by LDD-1819 or two small molecule inhibitors of glycogen synthase kinase-3β and aurora kinase A (BIO and reversine) and gene expression data for the myoblast markers Pax-7 and Myf5, 2) Cell viability of hTERT human immortalized fibroblasts, colon cancer cells and breast cancer cells, and 3) Western blotting analysis of full length and cleaved caspse-7, and cleaved poly (ADP-ribose) polymerase (PARP) in hTERT fibroblasts treated with LDD-1819. A schematic diagram of the biological activities of LDD-1819 is also presented. Further interpretation and discussion of these data are provided in the associated research article ‘A novel indirubin derivative that increases somatic cell plasticity and inhibits tumorigenicity’ (Kim et al., 2019).

Highlights

  • 4) Quantitative PCR analysis of gene expression related to myogenesis, apoptosis or cancer cell invasion

  • Value of the data This data describes the chemical characterization of novel indirubin derivative, LDD-1819, which modulates cell plasticity and inhibits tumorigenicity

  • C2C12 murine skeletal myoblasts, HCT116 human colon cancer cells and MDA-MB-231 human breast cancer cells were cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal bovine serum (FBS), 100 units/mL penicillin and 100 mg/mL streptomycin (PenStrep)

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Summary

Reagents and antibodies

BIO ((20Z,30E)-6-Bromoindirubin-30-oxime), CelLyticTM M lysis buffer, (b-D-arabinofuranosyl) cytosine) (AraC), and TRI-SolutionTM were purchased from Sigma-Aldrich. Reversine was purchased from Santa Cruz Biotechnology, Inc. An antibody for PARP (catalogue number #9541) was purchased from Cell Signaling Technology. An antibody for PARP (catalogue number #9541) was purchased from Cell Signaling Technology An antibody recognizing both full length and cleaved caspase-7 (catalogue number #9492) was purchased from Cell Signaling Technology. An antibody for GAPDH was purchased from Santa Cruz Biotechnology, Inc (catalogue number sc-365062)

Synthetic procedure of LDD-1819
Analytical data of the compound
Cell culture
Cell toxicity assay
Western blotting analysis
Measurement of aurora kinase A inhibition
2.10. Measurement of GSK-3b kinase inhibition
2.11. Statistical analysis
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