2. Anti-infection Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR Cytoskeleton
  3. Parasite DNA/RNA Synthesis AMPK Clathrin
  4. NEU-4438

NEU-4438 是一种抗疟 (Antimalarial) 剂。NEU-4438 可抑制 DNA 合成，减少 AMPK-γ，增加 Clathrin 重链。NEU-4438 对布氏锥虫 (Trypanosoma brucei) 具有抗寄生虫活性。NEU-4438 可降低慢性 HAT小鼠模型中的锥虫组织载量。

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NEU-4438

NEU-4438 Chemical Structure

CAS No. : 2306305-57-5

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NEU-4438 相关抗体

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NEU-4438 is an antimalarial agent. NEU-4438 inhibits DNA synthesis, reduces AMPK-γ, and increases Clathrin heavy chain. NEU-4438 exhibits antiparasitic activity against Trypanosoma brucei. NEU-4438 reduces trypanosome tissue burden in a chronic HAT mouse model[1].

IC50 & Target[1]

Trypanosoma

 

体外研究
(In Vitro)

NEU-4438 (系列稀释；处理 6 h) 可诱导血流型 Trypanosoma brucei brucei Lister427 细胞产生延迟杀锥虫活性，经 6 h 处理后换无化合物培养基培养 48 h 的 DCC50 为 334 nM[1]。
NEU-4438 (159-1474 nM; 6 h) 可剂量依赖性地降低表达 Myc 标签化 AMPK-γ 和网格蛋白重链的布氏锥虫血流型细胞中 AMPK-γ 蛋白水平[1]。
NEU-4438 (150 nM; 6 h) 可抑制布氏锥虫布氏亚种 Trypanosoma brucei brucei Lister427 血流型细胞的核 DNA 合成，具体表现为 EdU 阳性细胞数量减少以及细胞核 EdU 信号强度降低[1]。

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

NEU-4438 相关抗体:

Western Blot Analysis[1]

Cell Line: bloodstream Trypanosoma brucei cells expressing Myc-tagged AMPK-γ and clathrin heavy chain
Concentration: 159 nM (DCC25); 1474 nM (DCC90)
Incubation Time: 6 h
Result: Reduced AMPK-γ protein levels 0.54-fold at DCC25 and 0.86-fold at DCC90 compared to vehicle-treated cells.
Increased clathrin heavy chain levels 0.19-fold at DCC25 and 0.36-fold at DCC90 nM compared to vehicle-treated cells.

Immunofluorescence[1]

Cell Line: bloodstream Trypanosoma brucei brucei Lister427 cells
Concentration: 150 nM
Incubation Time: 6 h
Result: Increased the fraction of trypanosomes with one basal body (1BB) and decreased the proportion of cells with two basal bodies (2BB), with a statistically significant difference in population distribution compared to vehicle-treated cells (p = 2.8×10-2, Pearson’s Chi-square test).
体内研究
(In Vivo)

NEU-4438 (120-150 mg/kg；每日；感染后第 1-7 天) 在慢性 HAT 小鼠模型中，可使感染后第 7 天的锥虫组织中位载量降低 100 倍以上[1]。

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

Animal Model: Swiss-Webster (Hsd:ND4) (female, 8-10 weeks old, 20-25 g, infected with 5×104 bioluminescent T. brucei AnTat1.1 AmLuc via inoculation)[1]
Dosage: 150 mg/kg (days 1-4 post-infection); 120 mg/kg (days 5-7 post-infection)
Administration: daily; days 1-7 post-infection
Result: Produced a 3.92-fold reduction in trypanosome tissue bioluminescence signal on day 3 post-infection (p = 6.8×10-3).
Reduced median total trypanosome tissue flux greater than 100-fold, with undetectable tissue infection in 3 out of 4 treated mice on day 7 post-infection.
Left detectable parasites in tissues of 2 out of 4 treated mice on day 14 post-infection.
分子量

426.52

Formula

C24H26N8
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

NEU-4438 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:

NEU-44382306305-57-5NEU4438NEU 4438ParasiteDNA/RNA SynthesisAMPKClathrinAMP-activated protein kinasenuclear DNA synthesisbloodstream Trypanosoma brucei brucei Lister427 cellstransferrin endocytosisAMPK-γchronic human African trypanosomiasisTrypanosoma bruceihaptoglobin-hemoglobin endocytosisbasal body maturationmouse modelpolypeptide synthesisInhibitorinhibitorinhibit

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