For research use only.

Catalog No.S7060 Synonyms: AGL 1872, EI 275

20 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.

Selleck's PP1 has been cited by 20 publications

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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 MYLGeY5kfGmxbjDhd5NigQ>? NVzRO2lIUW6qaXLpeIlwdiCxZjDNUHIhe3SrbYXsZZRm\CCLTD2yJJBzd2S3Y4Tpc44hcW5iSoXyb4F1KGOnbHzzMEBKSzVyPUCuOEDPxE1? NX;EOoFbOTFyMUKwNlE>
mouse NIH/3T3 cells NHq5fmRHfW6ldHnvckBie3OjeR?= NVy1flVSOC5yOD2yNEDPxE1? NWTNPIF{UW6qaXLpeIlwdiCxZjD2MXNz[yCyaH;zdIhwenmuYYTpc44h\XiycnXzd4VlKGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZZQhOC5yODD0c{AzOCC3TTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NGj3NHMyQDh2OUm3NS=>

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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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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID