7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR

Uses

Lck Inhibitor is a cell-permeable ATP-competitive inhibitor of Lck.

Definition

ChEBI: RK-24466 is a member of the class of pyrrolopyrimidines that is 7H-pyrrolo[2,3-d]pyrimidine substituted by amino, 4-phenoxyphenyl, and cyclopentyl groups at positions 4, 5 and 7, respectively. It is a potent inhibitor of Lck that inhibits Lck (64-509) and LckCD isoforms (IC50 of less than 1 and 2 nM, respectively). It has a role as a geroprotector and an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor. It is a primary amino compound, a pyrrolopyrimidine, an aromatic amine, an aromatic ether and a member of cyclopentanes.

General Description

A cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, selective, and ATP-competitive inhibitor of Lck (IC₅₀ at 5 μM ATP = <1 nM, 2 nM, 70 nM, 1.57 μM and 1.98 μM for lck_64-509 Y³⁹⁴, Lckcd pY³⁹⁴, Src, Kdr and Tie-2, respectively; IC₅₀ at 1 mM ATP = 16 μM, 66 nM, 126 nM, 420 nM and 5.18 μM for Lck_64-509 Y³⁹⁴, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC₅₀ = 3.2 μM, >33 μM, >50 μM and >50 μM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC₅₀<1-40 nM in Jurkat T cells) and in vivo (ED₅₀ = 4 mg/kg in mice, ip.)

Biochem/physiol Actions

Primary TargetLck?????? Y3

in vivo