Bisindolylmaleimide IX

A protein kinase inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Experimental

1
Supporting references
0
Contradictory references
0
AI-suggested references
0
Clinical trials

General information

Bisindolylmaleimide IX is a protein kinase C inhibitor derived from maleimide (ChEBI). It was shown to be active also against various other protein kinases and targeting a spectrum of biological processes (Gupta et al., 2021 and references therein). It was also observed to be active against SARS-CoV-2 and its 3C-like protease in vitro (Gupta et al., 2021).

Bisindolylmaleimide IX on PubChem


Synonyms

Ro 31-8220; BIM IX

 

Structure image - Bisindolylmaleimide IX

CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)CCCSC(=N)N


Supporting references

Link Tested on Impact factor Notes Publication date
Bisindolylmaleimide IX: A novel anti-SARS-CoV2 agent targeting viral main protease 3CLpro demonstrated by virtual screening pipeline and in-vitro validation assays
3CLpro Enzyme assay In vitro In silico
in silico; in vitro enzyme assay; Vero E6 cells 3.81

The compound was predicted to bind the SARS-CoV-2 3C-like protease by computational methods. It inhibited viral entry with IC50 of 28.18 µM and viral spread with IC50 of 381.5 µM in Vero E6 cells. In an enzymatic assay it inhibited the 3C-like protease with IC50 of ca. 113.7 µM.

Jan/14/2021