2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Metabolic Enzyme/Protease
  3. EGFR Akt Mitochondrial Metabolism
  4. STA-013

STA-013 是一种 EphB 酪氨酸激酶抑制剂。STA-013 显示出针对 EphB1 (IC50 = 0.69 µM)、EphB2 (IC50 = 1.73 µM) 和 EphB4 (IC50 = 1.02 µM) 酪氨酸激酶的潜在抑制效力。STA-013 的抑制了 EphB 磷酸化信号，同时增强了 p-AKT/AKT 信号提示其激活了胰岛素信号通路。STA-013 通过增强胰岛素受体 β 信号和降低心脏中 TGF-β 水平来抑制 EphB 酪氨酸激酶。STA-013 可用于研究 2 型糖尿病及其心脏并发症 (糖尿病心肌病)。

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STA-013

STA-013 Chemical Structure

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规格 价格 是否有货
5 mg ￥1912
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10 mg ￥3060
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25 mg 询价 询问价格 & 货期
50 mg 询价 询问价格 & 货期

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Customer Review

STA-013 相关抗体

Top Publications Citing Use of Products

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STA-013 is a EphB tyrosine kinase inhibitor. STA-013 shows promising potency against EphB1 (IC50 = 0.69 µM), EphB2 (IC50 = 1.73 µM), and EphB4 (IC50 = 1.02 µM) tyrosine kinases. STA-013 results a inhibition of the EphB phosphorylated signal, coupled with increased p-AKT/AKT signaling, to suggest insulin signaling activation. STA-013 inhibits EphB tyrosine kinase by enhancing insulin receptor beta (IRβ) signaling, and decreasing TGF-β levels in the heart. STA-013 can be used for the study of type 2 diabetes and cardiac complications (diabetic cardiomyopathy)[1].

IC50 & Target[1]

ErbB1

0.69 μM (IC50)

ErbB2

1.73 μM (IC50)

ErbB4

1.02 μM (IC50)

体外研究
(In Vitro)

STA-013 (5 µM) 通过激酶组谱分析测定可抑制 EphB1 (54%)、EphB2 (42%)、EphB4 (52%)、SGK1 (47%) 和 PKBb (43%) 的活性，而对其余 140 种激酶无影响[1]。
STA-013 (0.032-20 µM, 96 h) 在胚胎小鼠 3T3-L1 细胞中以剂量依赖性方式显著抑制脂质积累[1]。
STA-013 (1 µM, 30 min) 导致 3T3-L1 细胞的基础呼吸、质子漏、ATP 产量和非线粒体耗氧量显著降低，增加最大呼吸和备用呼吸能力，糖酵解和糖酵解能力显著增强，并降低棕榈酸氧化水平[1]。

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

STA-013 相关抗体:
体内研究
(In Vivo)

STA-013 (12.5、25 和 50 mg/kg，腹腔注射，每日一次，持续 6 周) 在高脂饮食诱导的 C57BL/6 J 小鼠中可促进体重减轻改善葡萄糖清除和胰岛素敏感性，改善离体棕色脂肪组织和肝脏中的胰岛素信号传导[1]。
STA-013 (12.5、25 和 50 mg/kg，腹腔注射，每日一次，持续 6 周) 在 DIO 小鼠中诱导的体重减轻并非通过减少食物摄入或提高代谢率实现[1]。

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

Animal Model: HFD (for 10 weeks) induced male C57BL/6J mice (16-20 weeks old)[1]
Dosage: 12.5, 25 and 50 mg/kg
Administration: i.p., daily for 6 weeks
Result: Showed a significant reduction in whole-body weight, improved glucose clearance in the IP glucose tolerance test (GTT), and insulin sensitivity in the IP insulin tolerance test (ITT).
Showed a significant reduction in the fat mass associated with preserving the lean muscle mass in HFD-obese mice.
Induced intrascapular brown adipose tissue (BAT)-specific thermogenesis in HFD obese mice.
Showed significant reduction in whole-body weight associated with reduction in the fat mass (%) as well as increase in the lean mass (%), improved glucose clearance, and restored insulin sensitivity in HFD obese mice.
Inhibited phosphorylation of ephb tyrosine kinase forward signaling in both the liver and BAT at 25 mg/kg.
Increased the p-AKT/AKT signaling, which suggests the activation of insulin signaling in BAT and liver in HFD obese mice.
Increased insr-β protein levels compared to vehicle in BAT and liver lysates.
Animal Model: HFD (for 10 weeks) induced male C57BL/6J DIO mice (16-20 weeks old)[1]
Dosage: 12.5, 25 and 50 mg/kg
Administration: i.p., daily for 6 weeks
Result: Significantly increased oxygen (VO 2 and carbon dioxide (VCO 2) consumption ) production in the light cycle.
Decreased profile in the respiratory exchange rates (RER) during the dark cycle.
Decrease in the total energy expenditure (EE) for STA- 013 treated HFD mice.
Induced weight loss occurred without a change in food intake, suggesting it was due to an elevated metabolic rate.
分子量

411.48

Formula

C24H17N3O2S
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

STA-013 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

STA-013STA013STA 013EGFRAktMitochondrial MetabolismEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BEphBglucose homeostasisinsulin resistanceTGF-βtype 2 diabetescardiac complicationsInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-179572
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