Compound class:
Synthetic organic
Comment: S1g-2 is a small molecule that binds to heat shock protein 70 (Hsp70) and disrupts its regulatory interaction with the pro-apoptotic protein BCL2 like 11 (a.k.a. Bim; BCL2L11) [2]. S1g-2 is used as an experimental tool to demonstrate the potential antitumour effect of inhibiting the Hsp70/Bim interaction in therapy resistant cancers [2-4]. The ligand binds within Hsp70's nucleotide-binding domain (NBD) [2] at a site that is distinct from that of the allosteric anticancer compound MKT-077 (PubChem CID 6912334) [1].
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Bioactivity Comments |
S1g-2 inhibits the Hsp70/Bim interaction with an IC50 of 400 nM in a fluorescence polarization assay, using Hsp70 (isoform unspecified) nucleotide-binding domain (NBD; residues 1-383) [2]. |