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

SF-3-030 是一种强效、选择性且非 ATP 竞争性的 ERK1/2 抑制剂。SF-3-030 在携带突变型 BRaf 且 ERK1/2 信号通路持续活化的黑色素瘤细胞中，选择性地诱导细胞凋亡 (apoptosis)。SF-3-030 在哮喘的鼠类模型中缓解多种哮喘的病理特征。SF-3-030 可用于哮喘和黑色素瘤的研究。

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SF-3-030

SF-3-030 Chemical Structure

CAS No. : 1883721-73-0

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SF-3-030 相关抗体

Top Publications Citing Use of Products

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

SF-3-030 (2.5-60 μM；30 分钟) 在体外选择性抑制 ERK2 介导的 c-Fos 上 F 位点依赖性 Thr325 残基的磷酸化，对含有 D 结构域的底物 (RSK1) 或 p38α 介导的 ATF2 磷酸化无影响[2]。
SF-3-030 (1-100 μM；20 分钟-5 小时) 抑制 EGF/PMA 刺激的 HeLa/HEK293 细胞中的 AP-1 和 SRE 启动子活性，并抑制 A375 黑色素瘤细胞中的基础 AP-1 活性，对 PMA 诱导的反应表现出比对 EGF 诱导的反应更强的效力[2]。
SF-3-030 (5-100 μM；30 分钟-1 小时) 选择性抑制 EGF/PMA (HY-18739) 诱导的 HeLa 和 A375 细胞中含 F-位点的即刻早期基因 (c-Fos, Fra1, FosB, FosB2, c-Myc) 的表达，对非 F-位点即刻早期基因 (c-Jun, Egr1) 的影响最小[2]。
SF-3-030 (1-100 μM；24 小时) 选择性抑制具有组成型 ERK1/2 活性的黑色素瘤细胞 (A375, RPMI7951) 的增殖并诱导其凋亡，其 GI50 值分别为 7.1 和 4.6 μM，而在 Jurkat 细胞中表现出选择性，其 GI50 > 50 μM)[2]。

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

SF-3-030 相关抗体:

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.
体内研究
(In Vivo)

SF-3-030 (10 mg/kg; i.n.; 在每次 HDM 刺激前 30 分钟给药；每周 5 天，持续 3 周) 可减轻屋尘螨 (HDM) 诱导的小鼠哮喘模型的多项病理特征[1]。

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.
分子量

324.37

Formula

C14H12O5S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SF-3-030 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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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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