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MP-16   Click here for help

GtoPdb Ligand ID: 14310

Compound class: Synthetic organic
Comment: MP-16 is a c-Myc-PROTAC [1]. It includes a double-stranded nucleotide to engage the c-MYC protein and the small molecule VH032 (attached to the 5' end of the reverse strand via a short linker) that binds to the VHL E3 ubiquitin ligase. The construct induces formation of a VHL/PROTAC/c-Myc ternary complex that leads to selective VHL-mediated proteosomal degradation of c-MYC.
The full chemical SMILES is not available.
Bioactivity Comments
MP-16 degrades c-MYC in HCC cell lines, with maximum degradation evident between 4-8 hours after exposure [1]. This effect translates to anti-tumour activity in these cell lines.
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
MYC proto-oncogene, bHLH transcription factor Hs None Binding - - - 1
PROTAC degrader [1]