MPT0G211

MPT0G211 is a novel potent, selective HDAC6 inhibitor with IC50 of 0.291 nM, displays >1,000-fold selectivity over other HDAC isoforms; significantly inhibits tau phosphorylation on Ser396, Ser404, and phosphorylated tau (p-tau) aggregation, significantly attenuates apoptosis induced by p-tau, inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins; ameliorates learning and memory impairment in animal models of Alzheimer's disease, reduces the amount of phosphorylated tau in the hippocampal CA1 region; also demonstrates antiproliferative activity against human multiple myeloma RPMI 8226, U266, and NCI-H929 cells with no effect on normal bone marrow cells.

Identifier

CONSO00299

Type

chemical

Author

Kristian Kolpeja

https://orcid.org/0000-0001-9661-5277

References

• pubmed:29844403

Cross-references

• cas:2151853-97-1
• inchi:InChI=1S/C17H15N3O2/c21-17(20-22)14-8-6-12(7-9-14)11-19-15-5-1-3-13-4-2-10-18-16(13)15/h1-10,19,22H,11H2,(H,20,21)
• smiles:C1=CC(=CC=C1CNC2=CC=CC3=C2N=CC=C3)C(=O)NC

Synonyms

None available.

Incoming Relations

None available.

Outgoing Relations

None available.