| Bioactivity | 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]. |
| Invitro | 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]. Cell Cytotoxicity Assay[1] Cell Line: |
| 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) |
| Name | HSP90-IN-9 |
| Formula | C30H31N3O5 |
| Molar Mass | 513.58 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yin W, et al. Species-Selective Targeting of Fungal Hsp90: Design, Synthesis, and Evaluation of Novel 4,5-Diarylisoxazole Derivatives for the Combination Treatment of Azole-Resistant Candidiasis. J Med Chem. 2022, 65(7):5539-5564. |