ZM39923 hydrochloride

SKU: orb1227140

Description

ZM39923 is a potent, selective JAK3 inhibitor with pIC50 of 7.1, also potently inhibits human tissue transglutaminase (TGM2) with IC50 of 10 nM; ZM39923 is less potent for EGFR, JAK1 and CDK4 with pIC50 of 5.6, 4.4 and < 5.0, no activity fgor JAK2; alteres TGM2 activity in polyglutamine-expressing Drosophila model of neurodegeneration and is found to improve survival; significantly attenuates CCR7-induced Jak3 phosphorylation in metastatic SCCHN cells.

Key Properties

• CAS Number: 1021868-92-7
• MW: 367.9117
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₆ClNO
• SMILES: CC(C)N(CCC(=O)C1=CC2=CC=CC=C2C=C1)CC3=CC=CC=C3.Cl
• Target: JAK
• Solubility: DMSO: ≥ 47 mg/mL

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ZM-39923 hydrochloride

Quick Database Links

Gene Symbol

JAK