Description
WHI-P258 is a quinazoline compound that modeling studies suggested would bind to the active site of JAK3 with an estimated K
i value of 72 μM. However, it is inactive at JAK3 (IC
50 = >300 μM) and has been used as a negative control for structurally similar compounds that inhibit platelet aggregation and herpes simplex virus 1 (HSV-1) replication.
References
[1] E A SUDBECK. Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.[J]. Clinical Cancer Research, 1999, 5 6: 1569-1582.
[2] SHIN-ICHI YOKOTA . Induction of suppressor of cytokine signaling-3 by herpes simplex virus type 1 confers efficient viral replication[J]. Virology, 2005, 338 1: Pages 173-181. DOI:
10.1016/j.virol.2005.04.028[3] H. TIBBLES. Role of a JAK3-dependent Biochemical Signaling Pathway in Platelet Activation and Aggregation*[J]. The Journal of Biological Chemistry, 2001, 25 1: 17815-17822. DOI:
10.1074/jbc.m011405200