RP107

Chemical Properties

Yellow solid

Uses

A cell-permeable pyrrolo-pyrazine compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks: IC50 =150nM, 120 nM, 400 nM and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25,

Definition

ChEBI: 4-(7-butyl-1,5-dihydropyrrolo[2,3-b]pyrazin-6-ylidene)-1-cyclohexa-2,5-dienone is a member of quinomethanes.

General Description

A cell-permeable pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks; IC₅₀ = 150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively), glycogen synthase kinase-3 (GSK-3; IC₅₀ = 500 nM and 1.5 μM for GSK-3α, GSK-3β, respectively), and c-Jun N-terminal kinase (JNK; IC₅₀ = ~ 3 - 10 μM). It inhibits several other enzymes (CK1, CK2, MAPKK, PKA, PKG, PKCs, and c-raf) poorly (IC₅₀ ≥ 100 μM). Shown to arrest cells in both G₁ and G₂ phases (IC₅₀ = 7 μM and 10.5 μM for undifferentiated human teratocarcinoma cells NT2 and differentiated postmitotic neurons hNT, respectively). Shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 μM Forskolin (Cat. No. 344270) with high affinity (EC₅₀ = 150 nM, 140 nM and 111 nM, respectively).

Biochem/physiol Actions

EC50 = 150 nM, 140 nM and 111 nM, in stimulating CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 μM Forskolin, respectively