2. Anti-infection Epigenetics Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. Fungal HDAC Cytochrome P450
  4. CYP51/HDAC-IN-1

CYP51/HDAC-IN-1 是一种有效的，具有口服活性的 CYP51/HDAC 双重抑制剂。CYP51/HDAC-IN-1 抑制重要的毒力因子并下调相关耐药基因的表达。CYP51/HDAC-IN-1 对热带念珠菌病和隐球菌性脑膜炎均有有效的研究作用。

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CYP51/HDAC-IN-1 Chemical Structure

CYP51/HDAC-IN-1 Chemical Structure

CAS No. : 2502095-64-7

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CYP51/HDAC-IN-1 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target

CYP51

 

体外研究
(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].

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

CYP51/HDAC-IN-1 相关抗体:
体内研究
(In Vivo)

CYP51/HDAC-IN-1 (20 mg/kg; p.o.; once a day for 5 consecutive days) exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis (CM)[1].

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

Animal Model: Female ICR mice, 4-6 weeks, 18-20g (injection with C. tropicalis and C. neoformans via tail vein)[1]
Dosage: 20 mg/kg
Administration: p.o.; once a day; 5 consecutive days
Result: Reduced kidney fungal burden and brain fungal burden.
分子量

586.67

Formula

C30H40F2N6O4
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

CYP51/HDAC-IN-1 相关分类

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The molarity calculator equation

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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:

CYP51/HDAC-IN-12502095-64-7FungalHDACCytochrome P450Histone deacetylasesCYPsCandida tropicalisCryptococcus neoformansIFIs mouse modelslow toxicitybiofilm formationfungal ergosterolInhibitorinhibitorinhibit

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