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

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 Chemical Structure

CAS No. : 516-21-2

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Other Forms of Cycloguanil:

Cycloguanil Related Antibodies

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Description

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 3
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]
BC IC50
>50 3
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 3
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 3
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
>100 3
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
0.55 3
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]
HeLa EC50
0.55 3
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]
HeLa EC50
0.55 3
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]
HeLa EC50
> 100 3
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]
KB IC50
41 3
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 3
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]
HeLa EC50
> 100 3
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]
MDCK CC50
52 3
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 3
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 IC50
>50 3
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]
KB IC50
41 3
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 3
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 3
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 3
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 3
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 3
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 3
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 EC50
> 100 3
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 IC50
> 50 3
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]
In Vitro

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 Related Antibodies
Masse moléculaire

251.72

Formule

C11H14ClN5
CAS No.
SMILES

NC1=NC(N)=NC(C)(C)N1C2=CC=C(Cl)C=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
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Cycloguanil Related Classifications

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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:

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

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