1. Protein Tyrosine Kinase/RTK Immunology/Inflammation
  2. Src Interleukin Related
  3. LDDN-0003499

LDDN-0003499 是一种 Src 家族酪氨酸激酶抑制剂及抗炎剂。LDDN-0003499 可降低小胶质细胞中基础状态及 Aβ 刺激下的活化型磷酸化 LynSrc 激酶水平,并减弱 Aβ 刺激促炎细胞因子 TNFαIL-6 的分泌。LDDN-0003499 可用于阿尔茨海默病的相关研究。

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LDDN-0003499

LDDN-0003499 Chemical Structure

CAS No. : 331662-51-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LDDN-0003499 is a Src family tyrosine kinase inhibitor and anti-inflammatory agent. LDDN-0003499 reduces basal and Aβ-stimulated levels of active, phosphorylated Lyn and Src kinases, and attenuates Aβ-stimulated secretion of pro-inflammatory cytokines TNFα and IL-6 in microglial cells. LDDN-0003499 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

IL-6

 

体外研究
(In Vitro)

LDDN-0003499 (0.5 nM-50 μM; 24 h) 对小鼠小胶质细胞 BV2 无毒性[1]
LDDN-0003499 (0.5 nM-50 μM; 1 h) 可剂量依赖性地降低小鼠小胶质细胞 BV2 中的总蛋白磷酸酪氨酸水平[1]
LDDN-0003499 (0.5 nM-50 μM; 1 h) 可剂量依赖性地抑制小鼠小胶质细胞 BV2 中基础活性的磷酸化 LynSrc 水平[1]
LDDN-0003499 (0.5 nM-50 μM;65 min) 可在小鼠小胶质细胞 BV2 中呈剂量依赖性地抑制 Aβ 诱导的活化磷酸化 LynSrc 水平升高[1]
LDDN-0003499 (0.5 nM-50 μM; 1 h) 可呈剂量依赖性降低小鼠小胶质细胞 BV2 中 Aβ 刺激诱导的 TNF-α 和 IL-6 分泌[1]
LDDN-0003499 (1 μM) 在人源和小鼠肝微粒体中表现出中等偏高的 NADPH 依赖性清除率和较低的非 NADPH 依赖性清除率[1]

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

Western Blot Analysis[1]

Cell Line: unstimulated murine microglial BV2 cells
Concentration: 0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM, 50 μM
Incubation Time: 1 h
Result: Produced a dose-dependent decrease in active, phosphorylated Lyn (pLyn) and Src (pSrc) protein levels.
Did not alter phosphorylated levels of ERK, JNK, or p38.

Western Blot Analysis[1]

Cell Line: Aβ-stimulated murine microglial BV2 cells
Concentration: 0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM, 50 μM
Incubation Time: 1 h (pre-incubation); 5 min (co-incubation with 1 μM Aβ1-42)
Result: Attenuated the Aβ-stimulated increase in active, phosphorylated Lyn and Src protein levels.
Significantly attenuated the Aβ-stimulated increase in pLyn at 50 nM, while 500 nM was required for pSrc, demonstrating 10-fold selectivity for Lyn over Src in this paradigm.
Did not inhibit Aβ-stimulated increases in phosphorylated ERK.
分子量

350.20

Formula

C16H13Cl2N3O2

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
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  • 稀释计算器

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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.

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产品名称:
LDDN-0003499
目录号:
HY-112369
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