TR-07
TR-07 is a PRMT1 activator. TR-07 binds to the αY helix near the catalytic core to enhance PRMT1 homodimerization and catalytic activity, induces apoptosis in pancreatic cancer cells, and reduces cell viability. TR-07 can be used for research on pancreatic ductal adenocarcinoma and pancreatic cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C20H21N3O2
- Masse moléculaire:335.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
PRMT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PANC-1 | IC50 |
45 μM
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Cytotoxicity against human PANC-1 pancreatic tumor cells assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay.
Cytotoxicity against human PANC-1 pancreatic tumor cells assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay.
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42720487 |
In Vitro
TR-07 (100 μM; 2 h) selectively enhances the catalytic activity of PRMT1 by 45% without affecting the activity of PRMT3, PRMT4, or PRMT6[1].
TR-07 (1-2 h) enhances the enzymatic activity of PRMT1 toward natural and physiologically relevant substrates such as histone H2A, H4, and GAR[1].
TR-07 (100 μM), as an activator of PRMT1, increases its catalytic activity by 45% at 100 μM, while having no significant effect on PRMT6[1].
TR-07 (0.028-120 μM; 96 h) exhibits low cytotoxicity in PANC-1 pancreatic tumor cells with an IC50 of 45 μM[1].
TR-07 (10-20 μM; 72 h) effectively increases global asymmetric dimethylarginine (ADMA) levels in PANC-1 pancreatic tumor cells at non-toxic concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 pancreatic tumor cells
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Concentration:10; 20 μM
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Incubation Time:72 h
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Result:Resulted in a concentration-dependent increase in global arginine methylation compared to DMSO-treated control cells.
In Vivo
TR-07 (2 weeks) treatment increases cellular ADMA levels in PANC-1 tumor xenografts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude mice (female, 9-15 weeks, 20-30 g, subcutaneous xenograft)[1]
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Dosage:150 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Significantly reduced tumor growth compared to the PBS control group.
Further significantly reduced tumor growth in combination with gemcitabine compared to monotherapies.
Elevated mean intensity ADMA levels in PANC-1 xenografts upon application, both as monotherapy and in combination with gemcitabine, compared to PBS or gemcitabine alone.
Exhibited no significant adverse or systemic toxic effects at the applied doses.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- CCK-8/WST-8 Cell Proliferation Assay
- MTT Cell Proliferation Assay
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Masse moléculaire 335.40
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Formule C20H21N3O2
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SMILES
CN(CC1=CC(C/N=C/C2=C(NC(C3=CC=CC=C32)=O)O)=CC=C1)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TR-07 Related Classifications
HY-189431 Related Classifications
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