For research use only.
Catalog No.S7060 Synonyms: AGL 1872,EI 275
CAS No. 172889-26-8
PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
Selleck's PP1 has been cited by 15 publications
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Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for inhibitors at indicated times in the presence or absence of the kinase inhibitor PP1. The percent change in FITC-dextran over controls is presented as a measure of EC monolayer permeability. Data are derived from two independent experiments performed in triplicate with comparable results.
J Virol 2011 85(5), 2296-303. PP1 purchased from Selleck.
PP1 attenuated DAVLBH-induced lysosomal degradation of internalized VE-cadherin. HUVECs pretreated with or without PP1 were treated with or without DAVLBH for 4 h. Quantification of BV9/LAMP colocalization is shown (n = 3). The data are presented as mean ± SEM. ***P < 0.001 compared with the control group; #P < 0.05 and ###P < 0.001 compared with the DAVLBH group (one-way ANOVA with Tukey's post hoc comparison). Scale bar, 20 µm.
Theranostics, 2018, 8(2):384-398. PP1 purchased from Selleck.
The expression of epithelial and mesenchymal markers FYN-depleted MDA-MB-231 (D) cells by western blotting. (E) Immunofluorescence analysis of vimentin and E-cadherin expression and the morphology and distribution of F-actin in FYN-transfected MCF10A and FYN-depleted MDA-MB-231 cells.
Oncol Rep, 2016, 36(2):1000-6. PP1 purchased from Selleck.
Purity & Quality Control
Choose Selective Src Inhibitors
|Description||PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.|
PP1 is a nano-molar inhibitor of Lck and FynT, inhibits anti-CD3-induced protein-tyrosine kinase activity in T cells (IC50, 0.5 μM), demonstrates selectivity for Lck and FynT over ZAP-70, and preferentially inhibits T cell receptor-dependent anti-CD3-induced T cell proliferation (IC50, 0. 5 μM) over non-T cell receptor-dependent phorbol 12-myristate 13-acetate/interleu-kin-2 (IL-2)-induced T cell proliferation. PP1 (1 μM) selectively inhibits the induction of the IL-2 gene, but not the granulocyte-macrophage colony-stimulating factor or IL-2 receptor genes. PP1 also inhibits Src (IC50, 170 nM) and Hck (IC50, 20 nM). PP1 is 50–100-fold less active in the inhibition of A-431 epidermal growth factor receptor autophosphorylation (IC50, 0.25 μM).  PP1 also inhibits Kit and Bcr-Abl tyrosine kinases with IC50 of ∼75 nM and 1 μM, respectively. PP1 completely abrogates the proliferation of M07e cells in response to SCF with IC50 of 0.5–1 μM. PP1 (1 μM) inhibits SCF-induced c-Kit autophosphorylation in intact cells and blocks the activation of mitogen-activated protein kinase and Akt. PP1 inhibits the activity of mutant constitutively active forms of c-Kit (D814V and D814Y) found in mast cell disorders, and triggers apoptosis in the rat basophilic leukemia cell line RBL-2H3 that expresses mutant c-Kit. PP1 reduces the constitutive activation of signal transducer and activators of transcription 5 and mitogen-activated protein kinase and triggeres apoptosis in FDCP1 cells expressing Bcr-Abl. 
|In vitro||DMSO||4 mg/mL (14.21 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||AGL 1872,EI 275|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00791843||Completed||Drug: Growth hormone releasing hormone/ placebo||Congestive Heart Failure||University of Pennsylvania||March 2004||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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