Lck Inhibitor III - CAS 1188890-30-3 - Calbiochem

A cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a Lck (lymphocyte specific kinase) inhibitor (IC₅₀ = 867 nM; [ATP] = 10 µM). Shown to block IL-2 release in Jurkat E6-1 T cell line (IC₅₀ = 1.27 µM) stimulated by CD3 cross-linking and PMA. Although less potent than Lck Inhibitor II (Cat. No. 428206), it exhibits much improved aqueous solubility (27 µg/ml in 50 mM PBS, pH 7.4, ionic strength 0.15 M) and in vivo bioavailability (F = 22%, p.o. and i.v. at 10 mg/kg).

A cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a Lck (lymphocyte specific kinase) inhibitor (IC₅₀ = 867 nM; [ATP] = 10 µM). Shown to block IL-2 release in Jurkat E6-1 T cell line (IC₅₀ = 1.27 µM) stimulated by CD3 cross-linking and PMA. Although less potent than Lck Inhibitor II (Cat. No. 428206), it exhibits much improved aqueous solubility (27 µg/ml in 50 mM PBS, pH 7.4, ionic strength 0.15 M) and in vivo bioavailability (F = 22%, p.o. and i.v. at 10 mg/kg).

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sabat, M., et al. 2006. Bioorg. Med. Chem. Lett.16, 5973.

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Toxicity: Regulatory Review (Z)