2. Cell Cycle/DNA Damage Epigenetics Anti-infection
  3. HDAC Parasite
  4. HDAC1-IN-12

HDAC1-IN-12 是一种恶性疟原虫 (Plasmodium falciparum) HDAC1 (PfHDAC1) 抑制剂，其对恶性疟原虫的 IC50 为 4.1 nM。该抑制剂可抑制 PfHDAC1，上调恶性疟原虫 (P. falciparum) 寄生虫中组蛋白 H3 的乙酰化水平，下调疟疾入侵相关基因的表达，并具有良好的安全性特征、改善的理化性质和有效的体内抗疟活性。HDAC1-IN-12 可用于疟疾研究 。

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HDAC1-IN-12

HDAC1-IN-12 Chemical Structure

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HDAC1-IN-12 相关抗体

Top Publications Citing Use of Products

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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

HDAC1-IN-12 is a Plasmodium falciparum HDAC1 (PfHDAC1) inhibitor with an IC50 of 4.1 nM against Pf3D7. HDAC1-IN-12 inhibits PfHDAC1, upregulates histone H3 acetylation in P. falciparum parasites, downregulates malaria invasion-related gene expression, and exhibits favorable safety profiles, improved physicochemical properties, and potent in vivo antimalarial activity. HDAC1-IN-12 can be used for the research of malaria[1].

体外研究
(In Vitro)

HDAC1-IN-12 (compound 5ac) (72 h) 能强效抑制恶性疟原虫 (P. falciparum) 3D7 的生长，且对人源 HepG2 和 HEK293T 细胞具有高选择性 (恶性疟原虫 3D7 的 IC50 为 4.1 nM，HepG2 为 1.5 μM，HEK293T 为 15 μM)[1]。
HDAC1-IN-12 (72 h；6 h) 对多药耐药性恶性疟原虫 (P. falciparum) 菌株仍保持活性，并能抑制青蒿素耐药性环状期寄生虫 (GB4 的 IC50 为 3.9 nM，CP286 为 6 nM，6267 为 5.3 nM)[1]。
HDAC1-IN-12 (5 nM、50 nM；3 h) 可提高恶性疟原虫 (P. falciparum) 组蛋白 H3 的乙酰化水平[1]。
HDAC1-IN-12 (5-50 nM；3 h) 可下调侵袭相关基因，并阻断恶性疟原虫 (P. falciparum) 的裂解释放与红细胞侵袭[1]。

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

HDAC1-IN-12 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat[1] 1 mg/kg i.v. Cmax 91.2 ng/mL
Rat[1] 1 mg/kg i.v. Tmax 0.08 h
Rat[1] 1 mg/kg i.v. AUClast 47.9 ng·h/mL
Rat[1] 1 mg/kg i.v. AUCinf 48.5 ng·h/mL
Rat[1] 1 mg/kg i.v. T1/2 0.63 h
Rat[1] 10 mg/kg i.p. Cmax 143 ng/mL
Rat[1] 10 mg/kg i.p. Tmax 0.67 h
Rat[1] 10 mg/kg i.p. AUClast 237 ng·h/mL
Rat[1] 10 mg/kg i.p. AUCinf 239 ng·h/mL
Rat[1] 10 mg/kg i.p. T1/2 4.03 h
Rat[1] 10 mg/kg i.p. F 49.4 %
Rat[1] 10 mg/kg i.g. Cmax 10.2 ng/mL
Rat[1] 10 mg/kg i.g. Tmax 0.58 h
Rat[1] 10 mg/kg i.g. AUClast 29.7 ng·h/mL
Rat[1] 10 mg/kg i.g. AUCinf 34.3 ng·h/mL
Rat[1] 10 mg/kg i.g. T1/2 2.32 h
Rat[1] 10 mg/kg i.g. F 7.1 %
体内研究
(In Vivo)

HDAC1-IN-12 (compound 5ac) (30 mg/kg；腹腔注射；每日；连续 4 天) 在感染伯氏疟原虫 (Plasmodium berghei) ANKA 株的 BALB/c 小鼠模型中表现出明确的体内抗疟活性[1]。

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

Animal Model: BALB/c mice (female, 6–8 weeks old) were inoculated with 105 P. berghei ANKA\r\nparasite-infected erythrocytes via intraperitoneal injection (i.p.) on\r\nday 0.[1]
Dosage: 30 mg/kg
Administration: i.p.; daily; 4 days
Result: Showed no detectable parasitemia until day 11, with parasitemia levels remaining markedly lower than the DMSO control group.
分子量

467.50

Formula

C23H26FN7O3
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

HDAC1-IN-12 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

HDAC1-IN-12HDACParasiteHistone deacetylasesPlasmodium falciparum histone deacetylase 1histone H3 acetylationhuman HepG2 cellsPlasmodium falciparumGB4PfHDAC1artemisinin-resistant ring-stage parasitesP. falciparum egressPlasmodium berghei ANKA-infected model6267malaria invasion-related geneP. falciparum 3D7BALB/c miceHEK293T cellserythrocyte invasionmultidrug-resistant P. falciparum strainsQuisinostatP. falciparum histone H3P. falciparum parasitesCP286Inhibitorinhibitorinhibit

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目录号：
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