2. MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. ERK Apoptosis c-Myc
  4. 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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SF-3-030

SF-3-030 Chemical Structure

CAS No. : 1883721-73-0

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SF-3-030 Related Antibodies

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Description

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[1][2].

IC50 & Target[1][2]

ERK1

 

ERK2

 

In Vitro

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.

SF-3-030 Related Antibodies

Western Blot Analysis[2]

Cell Line: HeLa cells
Concentration: 5, 10, 20, 35, 40, 70, 100
Incubation Time: 30 min pretreatment
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.

Western Blot Analysis[2]

Cell Line: A375 melanoma cells
Concentration: 5, 25, 35, 50 μM
Incubation Time: 1 h
Result: Inhibited basal expression of c-Fos, FosB, FosB2, Fra1, and c-Myc but not Egr1.
In Vivo

SF-3-030 (10 mg/kg; i.n.; 30 min before each HDM challenge; 5 days a week for 3 weeks) mitigates multiple features of HDM-induced asthma in house dust mite (HDM) induced-mice[1].

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

Animal Model: Balb/c mice (8-10-week-old) challenged with HDM[1]
Dosage: 10 mg/kg
Administration: i.n.; 30 min before each HDM challenge; 5 days a week for 3 weeks
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.
Molecular Weight

324.37

Formula

C14H12O5S2
CAS No.
SMILES

O=S(=O)(OC1C=CS(=O)(=O)C1)C=2C=CC=3C=CC=CC3C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SF-3-030 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:

SF-3-0301883721-73-0ERKApoptosisc-MycExtracellular signal regulated kinasesMycERK1/2Ki-67house dust mite-induced asthmaA375 melanoma cellsp38αRSK1HDMmelanoma cellsATF2F-siteBALHeLa/HEK293 cellsmurine modelIgEc-JunFosB2Balb/c micecyclin D1mutated BRafFra1SREAP-1 transcription factor complexEgr1ERK1/2 substrate-docking domainsFosBDEF motifc-FosRPMI7951Inhibitorinhibitorinhibit

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