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.
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- CAS. Nr.: 2502095-64-7
- Formel: C30H40F2N6O4
- Molecular Weight:586.67
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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CYP51 |
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Cell Line
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Type | Value | Description | References |
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| 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] |
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.
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. Nr. 2502095-64-7
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Molecular Weight 586.67
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CYP51/HDAC-IN-1 Related Classifications
HY-144643 Related Classifications
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