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Tyrphostin A1

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Chemical Structure| 2826-26-8 同义名 : Tyrphostin 1;AG9
CAS号 : 2826-26-8
货号 : A630950
分子式 : C11H8N2O
纯度 : 99%+
分子量 : 184.194
MDL号 : MFCD00019787
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(570.05 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Tyrphostin A1 (AG9) is effective in inhibiting CD40L-stimulated IL-12 production in macrophage cultures and preventing the antigen-induced generation of Th1 cells. Its application leads to a dose-dependent reduction of IL-12 p40 levels, achieving maximum inhibition (62.5%) at a 10 μM concentration. Tyrphostin A1 also obstructs the CD40L-induced translocation of NF-κB to the nucleus and diminishes the activation of the IL-12 p40 gene. Therapeutic use of A1 in vivo results in decreased generation of myelin basic protein (MBP) specific encephalitogenic T cells and attenuates experimental allergic encephalomyelitis (EAE) in SJL/J mice, highlighting its potential for therapeutic applications in autoimmunity [1]. Compared to other tyrphostins, Tyrphostin A1 is a significantly weaker inhibitor of tyrosine kinase (TK), with an IC50 greater than 1250 μM for the epidermal growth factor receptor (EGFR) kinase, indicating its utility in distinguishing TK-mediated effects from non-specific actions of tyrphostins [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.43mL

1.09mL

0.54mL

27.15mL

5.43mL

2.71mL

54.29mL

10.86mL

5.43mL

参考文献

[1]Du C, et al. Inhibition of CD40 signaling pathway by tyrphostin A1 reduces secretion of IL-12 in macrophage, Th1 cell development and experimental allergic encephalomyelitis in SJL/J mice. J Neuroimmunol. 2001 Mar 1;114(1-2):69-79.

[2]Ogura T, et al. Activation of background membrane conductance by the tyrosine kinase inhibitor tyrphostin A23 and its inactive analog tyrphostin A1 in guinea pig ventricular myocytes. Jpn J Pharmacol. 2001 Nov;87(3):235-9.