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YC8-02

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Drug classSIRT2/3 inhibitor
PubChem CID
FormulaC46H63N3O2PS
YC8-02
Clinical data
Drug classSIRT2/3 inhibitor
Identifiers
  • 2-[[(2S)-1-(3-hydroxyanilino)-1-oxo-6-(tetradecanethioylamino)hexan-2-yl]amino]ethyl-triphenylphosphanium
PubChem CID
ChEMBL
Chemical and physical data
FormulaC46H63N3O2PS
Molar mass753.06 g·mol−1
3D model (JSmol)
  • CCCCCCCCCCCCCC(=S)NCCCC[C@@H](C(=O)NC1=CC(=CC=C1)O)NCC[P+](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4
  • InChI=1S/C46H62N3O2PS/c1-2-3-4-5-6-7-8-9-10-11-21-34-45(53)48-35-23-22-33-44(46(51)49-39-25-24-26-40(50)38-39)47-36-37-52(41-27-15-12-16-28-41,42-29-17-13-18-30-42)43-31-19-14-20-32-43/h12-20,24-32,38,44,47H,2-11,21-23,33-37H2,1H3,(H2-,48,49,50,51,53)/p+1/t44-/m0/s1
  • Key:RIVWUGLXBPHZGR-SJARJILFSA-O

YC8-02 is a drug which acts as a potent inhibitor of the enzymes sirtuin 2 (SIRT2) and sirtuin 3 (SIRT3). It was developed from an older SIRT2 selective inhibitor thiomyristoyl, but substituted with a triphenylphosphine group which increases affinity to SIRT3 and selectively targets uptake into mitochondria. It is still relatively selective for SIRT2 with an IC50 of 62nM at SIRT2 vs 530nM at SIRT3, but this still makes it one of the most potent SIRT3 inhibitors currently available. In animal studies it is useful for the treatment of certain forms of blood cancer such as lymphoma and leukemia.[1][2][3]

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