PP58是吡啶[2,3-d]嘧啶化合物，抑制PDGFR，FGFR和Src家族活性的IC₅₀值在纳摩尔级。

PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC 50 values.

Solid

PDGFR

PP58 inhibits Src with a subnanomolar IC50 value in the assays. PP58 behaves as a titration reagent at higher Src protein concentrations. As analyzed by immunoblotting with specific antiserum, the PP58 matrix specifically depletes Src from total lysate, whereas binding to the PP58 beads is prevented when free inhibitor is included. The ectopically expressed FGFR1 receptor tyrosine kinase is specifically retained on PP58 beads. PP58 matrix could be a novel affinity reagent for the purification of cellular pyrido[2,3-d]pyrimidine inhibitor targets. PP58 affinity chromatography leads to the identification of protein kinases belonging to various different groups and families, indicating that the pyrido[2,3-d]pyrimidine inhibitor is not selective for a set of phylogenetically related members of the human kinome. The Ki values of PP58 for p38α and JNK2 are 3.8±

PP58 can exhibit some degree of selectivity at low nanomolar concentrations in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Wissing J, et al. Chemical Proteomic Analysis Reveals Alternative Modes of Action for Pyrido[2,3-d]pyrimidine Kinase Inhibitors. Mol Cell Proteomics. 2004 Dec;3(12):1181-93.
[2]. Blencke S, et al. Characterization of a conserved structural determinant controlling protein kinase sensitivity to selective inhibitors. Chem Biol. 2004 May;11(5):691-701.

In Vitro: DMSO : 62.5 mg/mL (136.97 mM; Need ultrasonic)配制储备液