Tanzisertib

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Chemical Structure| 899805-25-5 同义名 : CC-930
CAS号 : 899805-25-5
货号 : A148034
分子式 : C21H23F3N6O2
纯度 : 98%
分子量 : 448.442
MDL号 : MFCD23160040
存储条件:

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(78.05 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

1M HCl: 100 mg/mL(222.99 mM),配合低频超声,并调节pH至1

动物实验配方:
生物活性
描述 Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin with an IC50 value of 1 μM[1]. At concentrations of 1-2 μM, Tanzisertib significantly diminishes hepatocyte apoptosis and necrosis, including in FC-loaded WT hepatocytes[2].
作用机制 CC-930 inhibits JNK1 and JNK2 in an ATP-competitive manner[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
Jurkat T cells Function assay Inhibition of JNK-mediated GST tagged c-Jun phosphorylation in human Jurkat T cells compound treated for 30 mins prior anisomycin stimulation measured after 40 mins by fluorescence spectrophotometry, IC50=0.2 μM 22244937
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.15mL

2.23mL

1.11mL

22.30mL

4.46mL

2.23mL

参考文献

[1]Lay T Gan, et al. Hepatocyte free cholesterol lipotoxicity results from JNK1-mediated mitochondrial injury and is HMGB1 and TLR4-dependent. J Hepatol. 2014 Dec;61(6):1376-84.

[2]Nicole Reich, et al. Jun N-terminal kinase as a potential molecular target for prevention and treatment of dermal fibrosis. Ann Rheum Dis. 2012 May;71(5):737-45.