HDAC/HSP90-IN-3

Names

[ CAS No. ]:
2700035-54-5

[ Name ]:
HDAC/HSP90-IN-3

Biological Activity

[Description]:

HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> HSP
Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Fungal
Signaling Pathways >> Cell Cycle/DNA Damage >> HSP
Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Signaling Pathways >> Epigenetics >> HDAC

[Target]

HSP90:0.83 μM (IC50, fungal Hsp90)

HDAC:0.91 μM (IC50, fungal HDACs)

human HDAC:3.0 μM (IC50, human HDACs)

HSP90:19.52 μM (IC50, human Hsp90)


[In Vitro]

HDAC/HSP90-IN-3 (compound J5) significantly down-regulates the adherence-related genes (such as ALS3, HWP1, EAP1, BCR1), and down-regulates the expression of ERG11 and CDR1[1].

[References]

[1]. Li C, Tu J, Han G, Liu N, Sheng C. Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans. Eur J Med Chem. 2022 Jan 5;227:113961.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H33N5O6

[ Molecular Weight ]:
511.57


Related Compounds