详情描述
ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
Product information
CAS Number: 1021868-92-7
Molecular Weight: 367.91
Formula: C23H26ClNO
Chemical Name: 3-[benzyl(propan-2-yl)amino]-1-(naphthalen-2-yl)propan-1-one hydrochloride
Smiles: Cl.CC(C)N(CC1C=CC=CC=1)CCC(=O)C1=CC2=CC=CC=C2C=C1
InChiKey: NJTUORMLOPXPBY-UHFFFAOYSA-N
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 47 mg/mL (127.75 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ZM39923 hydrochloride 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). 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. 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.
References:
- 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.
- 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.
- 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.
Products are for research use only. Not for human use.