SF-3-030
SF-3-030 is a potent, selective and non-ATP competitive ERK1/2 inhibitor. SF-3-030 selectively induces apoptosis in melanoma cells containing mutated BRaf and constitutively active ERK1/2 signalling. SF-3-030 mitigates multiple features of asthma in a murine model of asthma. SF-3-030 can be used for the research of asthma and melanomasup.
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- CAS No.: 1883721-73-0
- Formule: C14H12O5S2
- Masse moléculaire:324.37
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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ERK1 |
ERK2 |
SF-3-030 (2.5-60 μM; 30 min) selectively inhibits ERK2-mediated phosphorylation of the F-site-dependent Thr325 residue on c-Fos in vitro, with no effect on D-domain-containing substrates (RSK1) or p38α-mediated ATF2 phosphorylation[2].
SF-3-030 (1-100 μM; 20 min-5 h) inhibits AP-1 and SRE promoter activity in EGF/PMA-stimulated HeLa/HEK293 cells and suppresses basal AP-1 activity in A375 melanoma cells, showing greater potency against PMA-induced responses than against EGF-induced activity[2].
SF-3-030 (5-100 μM; 30 min-1 h) selectively inhibits EGF/PMA (HY-18739)-induced expression of F-site-containing IEGs (c-Fos, Fra1, FosB, FosB2, c-Myc) in HeLa and A375 cells, with minimal effect on non-F-site IEGs (c-Jun, Egr1)[2].
SF-3-030 (1-100 μM; 24 h) selectively inhibits proliferation and induces apoptosis in melanoma cells (A375, RPMI7951) with constitutive ERK1/2 activity, with GI50 values of 7.1 and 4.6 μM, respectively, while showing selectivity over Jurkat cells with a GI50 > 50 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:5, 10, 20, 35, 40, 70, 100
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Incubation Time:30 min pretreatment
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Result:Inhibited induction of c-Fos, FosB, FosB2, Fra1, and c-Myc in a dose-dependent manner in EGF-stimulated HeLa cells.
Showed less effect on c-Jun and Egr1 and inhibited c-Fos phosphorylation at Ser32 but not Ser374 in EGF-stimulated HeLa cells.
Inhibited c-Fos phosphorylation at Thr232 and Ser32 but not Ser374 and reduced FosB, FosB2, Fra1, and c-Myc expression
in PMA-stimulated HeLa cells.
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Cell Line:A375 melanoma cells
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Concentration:5, 25, 35, 50 μM
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Incubation Time:1 h
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Result:Inhibited basal expression of c-Fos, FosB, FosB2, Fra1, and c-Myc but not Egr1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice (8-10-week-old) challenged with HDM[1]
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Dosage:10 mg/kg
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Administration:i.n.; 30 min before each HDM challenge; 5 days a week for 3 weeks
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Result:Significantly attenuated HDM-induced airway inflammation.
Inhibited induction of airway remodeling (AR) by
repeated allergen challenge.
Inhibited the development of HDM-induced airway inflammation hyperresponsiveness (AHR).
Modulated gene expression profile in lung.
Modulated profile of proteins involved in multiple pathways in the lung.
Chemical Information
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CAS No. 1883721-73-0
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Masse moléculaire 324.37
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Formule C14H12O5S2
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SMILES
O=S(=O)(OC1C=CS(=O)(=O)C1)C=2C=CC=3C=CC=CC3C2
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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
[1]. Shah SD, et al. Targeted Inhibition of Select Extracellular Signal-regulated Kinases 1 and 2 Functions Mitigates Pathological Features of Asthma in Mice. Am J Respir Cell Mol Biol. 2023 Jan;68(1):23-38. [Content Brief]
[2]. Samadani R, et al. Small-molecule inhibitors of ERK-mediated immediate early gene expression and proliferation of melanoma cells expressing mutated BRaf. Biochem J. 2015;467(3):425-438. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- SF-3-030
- 1883721-73-0
- ERK
- Apoptosis
- c-Myc
- ERK1/2
- Ki-67
- house dust mite-induced asthma
- A375 melanoma cells
- p38α
- RSK1
- HDM
- melanoma cells
- ATF2
- F-site
- BAL
- HeLa/HEK293 cells
- murine model
- IgE
- c-Jun
- FosB2
- Balb/c mice
- cyclin D1
- mutated BRaf
- Fra1
- SRE
- AP-1 transcription factor complex
- Egr1
- ERK1/2 substrate-docking domains
- FosB
- DEF motif
- c-Fos
- RPMI7951
- Inhibitor
- inhibitor
- inhibit