货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S84405-5mg	≥98%	￥720.00 S84405-5mg ￥720.00 3-5天	0 货期：3-5天	-	-	-	-
S84405-10mg	≥98%	￥1170.00 S84405-10mg ￥1170.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S84405-5mg

≥98%

￥720.00

货期：3-5天

S84405-10mg

≥98%

￥1170.00

货期：3-5天

产品描述：

PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.

靶点：

PDGFR;FGFR; p38MAPK; TNF; PDGFR; Src

体外研究：

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±1.9 nM and 0.32±0.04 μM, respectively. PP58 affinity matrix also serves as an efficient purification reagent for a variety of protein kinases, which lack this structural feature and have much lower affinities for the pyrido[2,3-d]pyrimidine inhibitor PP58. PP58 inhibits anisomycin activated p38 in a dose-dependent manner with an IC50 below 10 nM. LPS-stimulated TNF-α production is potently inhibited by PP58 with a cellular IC50 value of around 3 nM. The T341M mutation abrogates the sensitivity to PP58 inhibition by increasing the cellular IC50 value of about 10 nM by more than 1000-fold. The cellular wild-type FGFR1 activity is potently inhibited by

体内研究：

PP58 can exhibit some degree of selectivity at low nanomolar concentrations in vivo

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.191 ml	10.957 ml	21.914 ml
5 mM	0.438 ml	2.191 ml	4.383 ml
10 mM	0.219 ml	1.096 ml	2.191 ml
50 mM	0.044 ml	0.219 ml	0.438 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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