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Tanzisertib

Tanzisertib (CC-930) 是有效的JNK1/2/3抑制剂，IC50分别为61、7 和 6 nM。

CAS号

899805-25-5

分子式

C21H23F3N6O2

主要靶点

JNK

仅限科研使用

Cat No : CM04920

Print datasheet

Synonyms

CC-930

验证数据展示

  • CAS No.: 899805-25-5

    Tanzisertib
    CAS#: 899805-25-5

产品信息

Tanzisertib (CC-930) is a potent inhibitor of JNK1/2/3 with IC50s of 61/7/6 nM, respectively, with potential antifibrotic activity.

CAS号 899805-25-5
分子式 C21H23F3N6O2
主要靶点 JNK
主要通路 MAPK信号通路
分子量 448.44
纯度 98.95%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 CC-930

靶点活性

JNK2:7 nM|JNK1:61 nM|JNK3:6 nM

体内活性

Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model[1]. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models. However, it can also induce the regression of pre-existing fibrosis[3].

体外活性

Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM)[1] and it blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis[3]. Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes[2].

溶解度

DMSO:33 mg/mL (73.59 mM)

参考文献

1.Plantevin Krenitsky V, et al. Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8.
2.Gan LT, 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.
3.Reich N, 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.
4.Tavernier SJ, et al. Regulated IRE1-dependent mRNA decay sets the threshold for dendritic cell survival. Nat Cell Biol. 2017 Jun;19(6):698-710.

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