2. Cell Cycle/DNA Damage Epigenetics Anti-infection
  3. HDAC Parasite
  4. FNDR-20123 free base

FNDR-20123 free base 是一种有效、安全、首创的抗疟疾 HDAC 抑制剂，对疟原虫和人类 HDAC 的 IC50 分别为 31 nM 和 3 nM。FNDR-20123 free base 对恶性疟原虫 (Plasmodium falciparum) 无性期 (IC50=41 nM) 和性血期 (雄性配子体 IC50=190 nM) 具有抗疟疾活性。FNDR-20123 free base 抑制 HDAC1，HDAC2，HDAC3，HDAC6，HDAC8 的 IC50 分别为 25，29，2，11，282 nM，并在纳摩尔浓度下抑制 III 类 HDAC 亚型。

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FNDR-20123 free base

FNDR-20123 free base Chemical Structure

CAS No. : 1267502-34-0

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FNDR-20123 free base 的其他形式现货产品:

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FNDR-20123 free base 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 Parasite 亚型特异性产品:

查看所有亚型
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations[1].

IC50 & Target[1]

human HDAC

3 nM (IC50)

Plasmodium HDAC

31 nM (IC50)

HDAC1

25 nM (IC50)

HDAC2

29 nM (IC50)

HDAC3

2 nM (IC50)

HDAC6

11 nM (IC50)

HDAC8

282 nM (IC50)

Plasmodium

 

体外研究
(In Vitro)

FNDR-20123 is active against all resistant strains tested so far, which will be highly valuable in eliminating the rapidly evolving drug-resistant parasite[1].

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

FNDR-20123 free base 相关抗体:
体内研究
(In Vivo)

FNDR-20123 (10-50 mg/kg; p.o.; bw for 4 days) is also able to reduce parasitaemia significantly in a mouse model for P. falciparum infection[1].

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

Animal Model: P. falciparum Pf3D70087/N9 in NODscidIL2Rγnull mice (engrafted with human erythrocytes)[1]
Dosage: 10 and 50 mg/kg
Administration: P.o.; bw for 4 days
Result: Resulted in a significant reduction in parasitaemia with 6.5% and 2.57% parasitaemia at 10 and 50 mg/kg, respectively.
分子量

377.44

Formula

C21H23N5O2
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

FNDR-20123 free base 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

FNDR-201231267502-34-0FNDR20123FNDR 20123HDACParasiteHistone deacetylasesresistantstrainsMDRsafeasexualmalegametocytesInhibitorinhibitorinhibit

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