ZM39923

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ZM39923 

ZM39923 是一种 JAK3 抑制剂, pIC50 值为 7.1;ZM39923 同时可抑制组织型转谷氨酞胺酶 (TGM2) 的活性,IC50 值为 10 nM。

ZM39923

ZM39923 Chemical Structure

CAS No. : 273727-89-2

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ZM39923 的其他形式现货产品:

ZM39923 hydrochloride

生物活性

ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.

IC50 & Target[1][2]

JAK3

7.1 (pIC50)

JAK1

4.4 (pIC50)

EGF-R

5.6 (pIC50)

Lck

5.0 (pIC50)

CDK4

5.0 (pIC50)

TGM2

10 nM (IC50)

体外研究
(In Vitro)

ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1. ZM39923 (Compound 7) shows weak inhibitory effect on EGF-R and JAK1 (pIC50, 5.6, 4.4, respectively), and insignificantly inhibits tyrosine kinases Lck and CDK4 (pIC50 <5.0)[1]. ZM39923 potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM, and acts directly on purified TGM2 to inhibit the Ca2+ activated form of TGM2[2]. ZM39923 blocks the phosphorylation of JAK3 induced by CCL19, and such an effect is similar to that of CCR7 antibody. ZM39923 also significantly blocks the CCL19 induced wound closure rate, and decreases the migration and invasion of PCI-37B cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

331.45

Formula

C23H25NO

CAS 号

273727-89-2

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.

参考文献
  • [1]. Brown GR, et al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000 Mar 20;10(6):575-9.

    [2]. Lai TS, et al. Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem Biol. 2008 Sep 22;15(9):969-78.

    [3]. Zhang Z, et al. Jak3 is involved in CCR7-dependent migration and invasion in metastatic squamous cell carcinoma of the head and neck. Oncol Lett. 2017 May;13(5):3191-3197.

Cell Assay
[3]

PCI-37B (a metastatic SCCHN cell line expressing CCR7) cells are cultured in Dulbecco’s modified Eagle’s medium (DMEM) containing 10% fetal bovine serum, penicillin, and streptomycin in an atmosphere of 5% CO2 and 95% air at 37°C. The ZM39923 inhibitor treatment at the dose determined using the Cell Counting Kit-8[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Brown GR, et al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000 Mar 20;10(6):575-9.

    [2]. Lai TS, et al. Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem Biol. 2008 Sep 22;15(9):969-78.

    [3]. Zhang Z, et al. Jak3 is involved in CCR7-dependent migration and invasion in metastatic squamous cell carcinoma of the head and neck. Oncol Lett. 2017 May;13(5):3191-3197.

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