ZM 39923 HClJAK3 inhibitor,potent and selective CAS# 1021868-92-7 |
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Quality Control & MSDS
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| Cas No. | 1021868-92-7 | SDF | Download SDF |
| PubChem ID | 176406 | Appearance | Powder |
| Formula | C23H26ClNO | M.Wt | 367.91 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 47 mg/mL (127.75 mM) H2O : 1 mg/mL (2.72 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-[benzyl(propan-2-yl)amino]-1-naphthalen-2-ylpropan-1-one;hydrochloride | ||
| SMILES | CC(C)N(CCC(=O)C1=CC2=CC=CC=C2C=C1)CC3=CC=CC=C3.Cl | ||
| Standard InChIKey | NJTUORMLOPXPBY-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H25NO.ClH/c1-18(2)24(17-19-8-4-3-5-9-19)15-14-23(25)22-13-12-20-10-6-7-11-21(20)16-22;/h3-13,16,18H,14-15,17H2,1-2H3;1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | ZM 39923 HCl is a potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3) with pIC50 value of 7.1. | |||||
| Targets | JAK3 | |||||
| IC50 | 7.1 (pIC50) | |||||
ZM 39923 HCl Dilution Calculator
ZM 39923 HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7181 mL | 13.5903 mL | 27.1806 mL | 54.3611 mL | 67.9514 mL |
| 5 mM | 0.5436 mL | 2.7181 mL | 5.4361 mL | 10.8722 mL | 13.5903 mL |
| 10 mM | 0.2718 mL | 1.359 mL | 2.7181 mL | 5.4361 mL | 6.7951 mL |
| 50 mM | 0.0544 mL | 0.2718 mL | 0.5436 mL | 1.0872 mL | 1.359 mL |
| 100 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.5436 mL | 0.6795 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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