1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Anti-infection
  2. HSP
    Fungal
  3. HSP90-IN-9

HSP90-IN-9 

Cat. No.: HY-145814
Handling Instructions

HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2).

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

HSP90-IN-9 Chemical Structure

HSP90-IN-9 Chemical Structure

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Description

HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2)[1].

IC50 & Target

HSP90

 

In Vitro

HSP90-IN-9 (compound A17) (combined with FLC (2 µg/mL)) shows antifungal activities against the six FLC-resistant Candida albicans (C. albicans) strains (MIC80s of 0.125 µg/mL in strain 901, strain 632, strain 100; MIC80s of 0.25 µg/mL in strain 904, strain 103,strain311, respectively)[1].
HSP90-IN-9 (24 h) shows low toxic to human cancer cells, human normal cells and the macrophage lineage (IC50s is 13.12, 34.09, 17.45, 7.15, >50, 21.33, 17.05, 10.34 µM in A549, MCF-7, HEPG2, THLE-2, BEAS-2B, NIH-3T3, Raw264.7, BV-2 cells, respectively)[1].
HSP90-IN-9 (32 μg/mL (combined with FLC (32 μg/mL)), 24 h) inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC[1].
HSP90-IN-9 (C. albicans (strain 904), 48 h) displays a fungicidal effect in a dose-dependent manner[1].
HSP90-IN-9 (FLC + compound A17 (32 + 32 μg/mL)) recovers azole sensitivity in resistant C.albicans by down-regulating the expression of CYP51 (ERG11) efflux pump-related genes (CDR1 and CDR2)[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: A549, MCF-7, HEPG2, THLE-2, BEAS-2B, NIH-3T3, Raw264.7, BV-2 cells
Concentration:
Incubation Time: 24 h
Result: Showed low toxic to human cancer cells, human normal cells and the macrophage lineage (IC50s of 13.12, 34.09, 17.45, 7.15, >50, 21.33, 17.05, 10.34 µM in A549, MCF-7, HEPG2, THLE-2, BEAS-2B, NIH-3T3, Raw264.7, BV-2 cells, respectively).

RT-PCR[1]

Cell Line: Azole-resistant strain 904
Concentration: 32 μg/mL (combined with FLC (32 μg/mL))
Incubation Time: 24 h
Result: Inhibited fungal biofilm formation and fungal morphological changes after being combined with FLC.
In Vivo

HSP90-IN-9 (10 mg/kg; i.v.) exhibits moderate pharmacokinetic properties in SD rats[1].
HSP90-IN-9 (A17 (10 mg/kg)+FLC (1 mg/kg); i.p.; once a day for 5 days) exhibits potent in vivo antifungal efficacy by reducing the colonization and dissemination of fungi in tissue[1].
Pharmacokinetic Parameters of HSP90-IN-9 in male Sprague-Dawley (SD) rats[1].

dose (mg/kg) T1/2 (h) C0 (ng/mL) AUC(0-t) (h*ng/mL) AUC(0-∞) (h*ng/mL) Vz (L/kg) Cl (mL/min/kg) MRT(0-∞) (h)
10 mg/kg 1.26±0.31 4752.50±44.54 3005.15±35.59 3028.95±54.14 11.25±3.69 101.77±1.96 1.12±0.07

male Sprague-Dawley (SD) rats; 10 mg/kg; i.v.[1]

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

Animal Model: male Sprague-Dawley (SD) rats[1]
Dosage: 10 mg/kg
Administration: i.v.
Result: Exhibited moderate pharmacokinetic properties in SD rats.
Animal Model: female SD rats, 160-180 g (IFI rat model)[1]
Dosage: 10 mg/kg, A17 (10 mg/kg)+FLC (1 mg/kg)
Administration: i.p., once a day, 5 days
Result: Exhibited potent in vivo antifungal efficacy by reducing the colonization and dissemination of fungi in tissue.
Molecular Weight

513.58

Formula

C30H31N3O5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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HSP90-IN-9
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HY-145814
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