1. Anti-infection
    Epigenetics
    Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. Fungal
    HDAC
    Cytochrome P450
  3. CYP51/HDAC-IN-1

CYP51/HDAC-IN-1 

Cat. No.: HY-144643
Handling Instructions

CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis.

For research use only. We do not sell to patients.

CYP51/HDAC-IN-1 Chemical Structure

CYP51/HDAC-IN-1 Chemical Structure

CAS No. : 2502095-64-7

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Description

CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis[1].

IC50 & Target

CYP51

 

In Vitro

CYP51/HDAC-IN-1 (compound A5) exhibits the best inhibitory activity against both Candida tropicalis (C. tropicalis) and Cryptococcus neoformans (C. neoformans) with an MIC80 of 0.5 µg/mL[1].
CYP51/HDAC-IN-1 (human umbilical vein endothelial cell line (HUVEC)) shows low toxicity to human normal cells (IC50= 5.9 µg/mL (10.36 µM))[1].
CYP51/HDAC-IN-1 inhibits biofilm formation of C. tropicalis and C. neoformans in a dose-dependent manner[1].
CYP51/HDAC-IN-1 reduces the virulence of C. neoformans through down-regulating capsule-associated genes CAP10 and CAP60[1].
CYP51/HDAC-IN-1 increases the activity against FLC-resistant C. tropicalis by inhibits the overexpression of efflux pump genes, and down-regulated ERG11 gene in ergosterol biosynthetic pathway[1].
CYP51/HDAC-IN-1 exhibits HDAC inhibitory activity (IC50=2.38 µM) and down-regulated HDAC genes (Rpd3, Hos1, Hos2, Clr61, Clr62, Hda1 and Hos3)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CYP51/HDAC-IN-1 (20 mg/kg; p.o.; once a day for 5 consecutive days) exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis (CM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female ICR mice, 4-6 weeks, 18-20g (injection with C. tropicalis and C. neoformans via tail vein)[1]
Dosage: 20 mg/kg
Administration: p.o.; once a day; 5 consecutive days
Result: Reduced kidney fungal burden and brain fungal burden.
Molecular Weight

586.67

Formula

C30H40F2N6O4

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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CYP51/HDAC-IN-1
Cat. No.:
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