2. Cell Cycle/DNA Damage Anti-infection Stem Cell/Wnt JAK/STAT Signaling
  3. Parasite DNA/RNA Synthesis STAT Antifolate
  4. Cycloguanil

Cycloguanil  (Synonyms: Chlorguanide triazine)

製品番号: HY-12784
取扱説明書 Technical Support

Cycloguanil (Chlorguanide triazine) is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Cycloguanil hydrochloride) usually boasts enhanced water solubility and stability.

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Cycloguanil

Cycloguanil 構造式

CAS 番号 : 516-21-2

容量 在庫状況
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100 mg   お問い合わせ  
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Other 在庫あり Forms of Cycloguanil:

Other Forms of Cycloguanil:

Cycloguanil 関連抗体

Top Publications Citing Use of Products

Parasite アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

STAT アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
STAT3 STAT5 STAT6 STAT1

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製品説明

Cycloguanil (Chlorguanide triazine) is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity[1][2].

IC50 & Target

Plasmodium

 

Cellular Effect
Cell Line Type Value Description References
BC IC50
>50 μM
Compound: Cycloguanil (C21)
In vitro cytotoxicity against Plasmodium falciparum infected BC cell line.
In vitro cytotoxicity against Plasmodium falciparum infected BC cell line.
[PMID: 14736247]
HeLa EC50
>100 μM
Compound: 1
Antiviral activity against coxsackie B4 virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against coxsackie B4 virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
HeLa EC50
>100 μM
Compound: 1
Antiviral activity against vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
HeLa EC50
0.55 μM
Compound: 1
Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
KB IC50
41 μM
Compound: Cycloguanil (C21)
In vitro cytotoxicity against Plasmodium falciparum infected KB cell line
In vitro cytotoxicity against Plasmodium falciparum infected KB cell line
[PMID: 14736247]
MDCK CC50
52 μM
Compound: 1
Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay
Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay
[PMID: 28477572]
Vero EC50
>100 μM
Compound: 1
Antiviral activity against Coxsackie B4 virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against Coxsackie B4 virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
Vero EC50
>100 μM
Compound: 1
Antiviral activity against para influenza 3 virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against para influenza 3 virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
Vero EC50
>100 μM
Compound: 1
Antiviral activity against Punta Toro virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against Punta Toro virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
Vero EC50
>100 μM
Compound: 1
Antiviral activity against Reovirus 1 infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against Reovirus 1 infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
Vero EC50
>100 μM
Compound: 1
Antiviral activity against Sindbis virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against Sindbis virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
Vero EC50
>100 μM
Compound: 1
Antiviral activity against Yellow fever virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
Antiviral activity against Yellow fever virus infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis
[PMID: 28477572]
Vero IC50
>50 μM
Compound: Cycloguanil (C21)
In vitro cytotoxicity against Plasmodium falciparum infected vero cell line.
In vitro cytotoxicity against Plasmodium falciparum infected vero cell line.
[PMID: 14736247]
体外実験

Cycloguanil exhibits anticancer activity against the NCI-60 panel of human tumor cell lines, and shows selective activity toward the MDA-MB-468 and MCF-7 breast cancer cell lines[2].
Cycloguanil (72 h) induces growth arrest in MDA-MB-468, MDA-MB-231 and MCF-7 breast cancer cells, with cell viability maintained at approximately 50% of that in the vehicle control group at high concentrations, and this effect cannot be reversed by folinic acid treatment[2].
Cycloguanil (0.001-10 μM; 24 h) binds to DHFR in intact MDA-MB-468 breast cancer cells, resulting in a dose-dependent accumulation of DHFR protein after 24 hours of treatment[2].
Cycloguanil (10 μM; 24 h) disrupts folate metabolism and nucleotide homeostasis in MDA-MB-231 breast cancer cells, and supplementation with Folinic acid (HY-17556) reverses the metabolite changes induced by it, a result consistent with DHFR inhibition[2].
Cycloguanil (0.02-20 μM; 6 h) potently inhibits the transcriptional activity of STAT3 in U3A fibrosarcoma cells at concentrations as low as 0.02 μM, which is consistent with the downstream effects of DHFR inhibition[2].

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

Cycloguanil 関連抗体
分子量

251.72

分子式

C11H14ClN5
CAS 番号
SMILES

NC1=NC(N)=NC(C)(C)N1C2=CC=C(Cl)C=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献
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Cycloguanil Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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:

Cycloguanil516-21-2Chlorguanide triazineParasiteDNA/RNA SynthesisSTATAntifolatemalaria schizontserythrocyteshuman DHFRMDA-MB-468folate metabolismhepatocytesSTAT3primary human hepatocytesOCT1nucleotide metabolismInhibitorinhibitorinhibit

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