ZM 39923 HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ZM 39923是JAK1和JAK3的选择性抑制剂,其pIC50值分别为4.4和7.1[1][2]。
JAK(Janus激酶)是细胞内非受体酪氨酸激酶家族的成员,通过JAK-STAT信号通路转导细胞因子介导的信号。实验表明,I型和II型细胞因子受体家族依赖JAK家族,以磷酸化并激活该信号转导途径的下游蛋白。鉴于JAK的生物活性,多种JAK抑制剂已被研发,主要用于筛选血液系统疾病、肿瘤、类风湿性关节炎和银屑病治疗药物[2][3]。
ZM 39923是JAK1和JAK3的选择性抑制剂。在类风湿性关节炎(RA)细胞中,ZM39923和Curcumol(50 μg/ml)联合用药可以分别抑制Jak3-Stat5通路相关分子活性以及Bcl-2表达,从而抑制CD4+T细胞增殖,诱导细胞凋亡[4]。在融合ARPE-19细胞中,ZM 39923预处理后给予丙烯醛处理通过介导JAK3和TGFβ2,从而降低细胞活力,增加VEGF表达[3]。
据报道,ZM39923抑制TGM2(被认为是治疗多种疾病的靶点),其IC50值为10 nM[5]。此外,ZM39923对EGFR具有同等的抑制作用[1]。
参考文献:
[1]. Luo, C. and P. Laaja, Inhibitors of JAKs/STATs and the kinases: a possible new cluster of drugs. Drug Discov Today, 2004. 9(6): p. 268-75.
[2]. Brown, G.R., et al., Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett, 2000. 10(6): p. 575-9.
[3]. Vidro-Kotchan, E., et al., NBHA reduces acrolein-induced changes in ARPE-19 cells: possible involvement of TGFbeta. Curr Eye Res, 2011. 36(4): p. 370-8.
[4]. Wang, H., et al., The molecular mechanism of curcumol on inducing cell growth arrest and apoptosis in Jurkat cells, a model of CD4(+) T cells. Int Immunopharmacol, 2014. 21(2): p. 375-82.
[5]. Lai, T.S., et al., Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries. Chem Biol, 2008. 15(9): p. 969-78.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 367.91 |
Cas No. | 1021868-92-7 |
Formula | C23H25NO·HCl |
Solubility | ≥7.74 mg/mL in EtOH with gentle warming and ultrasonic; ≥9.2 mg/mL in DMSO |
Chemical Name | 3-(benzyl(isopropyl)amino)-1-(naphthalen-2-yl)propan-1-one hydrochloride |
SDF | Download SDF |
Canonical SMILES | CC(C)N(CC1=CC=CC=C1)CCC(C2=CC3=CC=CC=C3C=C2)=O.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | ZM 39923 HCl是有效的Janus酪氨酸激酶3(JAK3)选择性抑制剂,其pIC50值为7.1。 | |||||
靶点 | JAK3 | |||||
IC50 | 7.1 (pIC50) |
质量控制和MSDS
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