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

HSP90-IN-9 是一种有效的选择性 HSP90 抑制剂。HSP90-IN-9 以剂量依赖性方式显示杀真菌作用。HSP90-IN-9 与 FLC 联合用药可抑制真菌生物膜形成和真菌形态变化。HSP90-IN-9 可通过下调 ERG11、CDR1 和 CDR2 基因表达恢复对 FLC 的耐药性。

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HSP90-IN-9 Chemical Structure

HSP90-IN-9 Chemical Structure

CAS No. : 2765247-36-5

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HSP90-IN-9 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
13.12 μM
Compound: A17
Cytotoxicity against human A549 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
Cytotoxicity against human A549 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
[PMID: 35298171]
BEAS-2B IC50
> 50 μM
Compound: A17
Cytotoxicity against human BEAS-2B cell assessed as inhibition of cell growth after 24 hrs by MTT assay
Cytotoxicity against human BEAS-2B cell assessed as inhibition of cell growth after 24 hrs by MTT assay
[PMID: 35298171]
BV-2 IC50
10.34 μM
Compound: A17
Cytotoxicity against mouse BV-2 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
Cytotoxicity against mouse BV-2 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
[PMID: 35298171]
HepG2 IC50
17.45 μM
Compound: A17
Cytotoxicity against human HepG2 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
[PMID: 35298171]
MCF7 IC50
34.09 μM
Compound: A17
Cytotoxicity against human MCF7 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
[PMID: 35298171]
NIH3T3 IC50
21.33 μM
Compound: A17
Cytotoxicity against mouse NIH3T3 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
Cytotoxicity against mouse NIH3T3 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
[PMID: 35298171]
RAW264.7 IC50
17.05 μM
Compound: A17
Cytotoxicity against mouse RAW264.7 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
[PMID: 35298171]
THLE-2 IC50
7.15 μM
Compound: A17
Cytotoxicity against human THLE-2 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
Cytotoxicity against human THLE-2 cell assessed as inhibition of cell growth after 24 hrs by MTT assay
[PMID: 35298171]
体外研究
(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.

HSP90-IN-9 相关抗体:

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.
体内研究
(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.
分子量

513.58

Formula

C30H31N3O5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HSP90-IN-9 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HSP90-IN-92765247-36-5HSPFungalHeat shock proteinsazole-resistant candidiasisantifungalselectiveIFI rat modelbiofilm formationmorphological changeslow toxicInhibitorinhibitorinhibit

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