ZM 39923 HCl
(Synonyms: 3-[异丙基(苄基)氨基]-1-(2-萘基)-1-丙酮盐酸盐) 目录号 : GC14245
A potent inhibitor of JAK3
Cas No.:1021868-92-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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]. |
References: [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. | |
ZM 39923 is a selective inhibitor of JAK1 and JAK3 with pIC50 value of 4.4 and 7.1, respectively [1] [2].
JAK (Janus kinase) is a member of intracellular, non-receptor tyrosine kinases family and plays a pivotal role in transducing cytokine-mediated signals via the JAK-STAT pathway. It has been shown that type I and type II cytokine receptor families rely on the JAK family to phosphorylate and activate downstream proteins involved in their signal transduction pathways. Considering the biological function of JAK, a veraity of JAK inhibitors have been developed and mainly used for screening blood system disease, tumor, rheumatoid arthritis and psoriasis treatment [2] [3].
ZM 39923 is a selective JAK1 and JAK3 inhibitor. When tested with RA cells, administration of ZM 39923 combined with 50 μg/ml curcumol suppressed CD4(+) T cell proliferation and induced apoptosis through inhibiting Jak3-STAT5-related molecular activities and Bcl-2 expression, respectively [4]. In confluent ARPE-19 cells, pretreated with ZM 39923 followed acrolein treatment resulted in the reduction of cell viability and increased VEGF expression via mediating JAK3 and TGFβ2 [3].
It is reported that ZM 39923 has the inhibitory effect on TGM2 (which considered as a target for several disease treatment) with the IC50 value of 10 nM [5] and the same effect on EGFR [1].
References:
[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.
| Cas No. | 1021868-92-7 | SDF | |
| 别名 | 3-[异丙基(苄基)氨基]-1-(2-萘基)-1-丙酮盐酸盐 | ||
| 化学名 | 3-(benzyl(isopropyl)amino)-1-(naphthalen-2-yl)propan-1-one hydrochloride | ||
| Canonical SMILES | CC(C)N(CC1=CC=CC=C1)CCC(C2=CC3=CC=CC=C3C=C2)=O.Cl | ||
| 分子式 | C23H25NO.HCl | 分子量 | 367.91 |
| 溶解度 | ≥ 9.2 mg/mL in DMSO, ≥ 7.74 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7181 mL | 13.5903 mL | 27.1806 mL |
| 5 mM | 0.5436 mL | 2.7181 mL | 5.4361 mL |
| 10 mM | 0.2718 mL | 1.359 mL | 2.7181 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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