Lck Inhibitor

• CAT Number: R064986
• CAS Number: 213743-31-8
• Molecular Formula: C23H22N4O
• Molecular Weight: 370.5
• Purity: ≥95%
• Synonyms: Lymphocyte-specific protein tyrosine kinase;RK-24466​
• Target: Src
• Storage: -20°C
• InChI: InChI=1S/C23H22N4O/c24-22-21-20(14-27(17-6-4-5-7-17)23(21)26-15-25-22)16-10-12-19(13-11-16)28-18-8-2-1-3-9-18/h1-3,8-15,17H,4-7H2,(H2,24,25,26)
• InChIKey: FMETVQKSDIOGPX-UHFFFAOYSA-N
• SMILES: NC1=C2C(C(C=C3)=CC=C3OC4=CC=CC=C4)=CN(C5CCCC5)C2=NC=N1

Lymphocyte-<wbr></wbr>specific protein tyrosine kinase (Lck) is a member of the Src-<wbr></wbr>family of non-<wbr></wbr>receptor protein tyrosine kinases and plays a critical role in the initial steps of T cell receptor signaling that trigger the production of cytokines. Lck inhibitor is a pyrrolopyrimidine that blocks the activity of two forms of Lck kinase, Lck (64-<wbr></wbr>509) and Lckcd, with IC50 values of <1 and 2 nM, respectively. It inhibits the related kinases Src, Kdr, and Tie-<wbr></wbr>2 with much weaker potency (IC50s = 70 nM, 1.57, and 1.98 µM, respectively) and only minimally inhibits the activities of EGFR, PKC, CDC2/B and ZAP-<wbr></wbr>70 (IC50s = 3.2, >33, >50, and >50 µM, respectively). This compound has been shown to inhibit T cell receptor-<wbr></wbr>stimulated IL-<wbr></wbr>2 production in mice (ED50s = 4 and 25 mg/kg when administered either i.p. or orally).

Reference

1.Khatik, R., and Pathak, A.K. Lck inhibitors and its analogues: A review. Der Pharma Chemica 3(2), 310-320 (2011).