For research use only.

Catalog No.S7060 Synonyms: AGL 1872, EI 275

17 publications

PP1 Chemical Structure

CAS No. 172889-26-8

PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

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Selleck's PP1 has been cited by 17 publications

4 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.

  • 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.

  • (a) Western blot shows that UUO dramatically induces Src activation in day 7 UUO kidney, which is effectively blocked in mice treated with Src inhibitor PP1 (2 mg/kg per day, i.p.).

    Kidney Int, 2018, 93(1):173-187. 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 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
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 NF\I[HZHfW6ldHnvckBie3OjeR?= NFzRSGdKdmirYnn0bY9vKG:oIF3MVkB{fGmvdXzheIVlKEmOLUKgdJJw\HWldHnvckBqdiCMdYLrZZQh[2WubIOsJGlEPTB;MD60JO69VQ>? MVWxNVAyOjB{MR?=
mouse NIH/3T3 cells MlXTSpVv[3Srb36gZZN{[Xl? M3SzfVAvODhvMkCg{txO NGX0[odKdmirYnn0bY9vKG:oII[tV5JkKHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhcW5ibX;1d4UhVkmKL{PUN{Bk\WyuczDheEAxNjB6IITvJFIxKHWPIHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? M1y0flE5QDR7OUex

... Click to View More Cell Line Experimental Data


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


CAS No. 172889-26-8
Storage powder
in solvent
Synonyms AGL 1872, EI 275
Smiles CC1=CC=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)(C)C

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID