CYP51/HDAC-IN-1
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.
- CAS No.: 2502095-64-7
- Formula: C30H40F2N6O4
- Molecular Weight:586.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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CYP51 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
5.9 μg/mL
Compound: A5
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Cytotoxicity against human HUVEC assessed as reduction in cell viability
Cytotoxicity against human HUVEC assessed as reduction in cell viability
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[PMID: 33992927] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female ICR mice, 4-6 weeks, 18-20g (injection with C. tropicalis and C. neoformans via tail vein)[1]
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Dosage:20 mg/kg
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Administration:p.o.; once a day; 5 consecutive days
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Result:Reduced kidney fungal burden and brain fungal burden.
Chemical Information
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CAS No. 2502095-64-7
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Molecular Weight 586.67
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Formula C30H40F2N6O4
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SMILES
O=C(CCCCCCCOC1=CC=C(CN2CCN(CC(C3=CC=C(C=C3F)F)(CN4N=CN=C4)O)CC2)C=C1)NO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CYP51/HDAC-IN-1 Related Classifications
HY-144643 Related Classifications
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