PP1

Catalog No.S7060 Synonyms: AGL 1872,EI 275

PP1 Chemical Structure

Molecular Weight(MW): 281.36

PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

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2 Customer Reviews

  • 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.

    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.

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Biological Activity

Description PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
Targets
LCK [1]
(Cell-free assay)
Fyn [1]
(Cell-free assay)
Kit [2]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
5 nM 6 nM ~75 nM 250 nM
In vitro

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). [1] 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. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat cells NGHwTplHfW6ldHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKE2OUjDzeIlufWyjdHXkJGlNNTJicILv[JVkfGmxbjDpckBLfXKtYYSgZ4VtdHNuIFnDOVA:OC52IN88US=> M2PqRlEyODF{MEKx
mouse NIH/3T3 cells MkHPSpVv[3Srb36gZZN{[Xl? NUPjW2p7OC5yOD2yNEDPxE1? MVvJcohq[mm2aX;uJI9nKHZvU4LjJJBpd3OyaH;yfYxifGmxbjDlfJBz\XO|ZXSgbY4hdW:3c3WgUmlJNzOWMzDj[YxteyCjdDCwMlA5KHSxIEKwJJVOKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MknPNVg5PDl7N{G=

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 4 mg/mL (14.21 mM)
Water Insoluble
Ethanol Insoluble

* 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.

Chemical Information

Molecular Weight 281.36
Formula

C16H19N5

CAS No. 172889-26-8
Storage powder
Synonyms AGL 1872,EI 275

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02431702 Recruiting Schizophrenia|Psychotic Disorders Janssen Scientific Affairs, LLC July 2015 Phase 3
NCT01515423 Completed Schizophrenia Janssen Research & Development, LLC May 2012 Phase 3

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID