PP1

Catalog No.S7060 Synonyms: AGL 1872, EI 275

For research use only.

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

PP1 Chemical Structure

CAS No. 172889-26-8

Selleck's PP1 has been cited by 21 publications

Purity & Quality Control

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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.
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 MoLTSpVv[3Srb36gZZN{[Xl? M4DkOGlvcGmkaYTpc44hd2ZiTVzSJJN1cW23bHH0[YQhUUxvMjDwdo9lfWO2aX;uJIlvKEq3cnvheEBk\WyuczygTWM2OD1yLkSg{txO NXzVUWo3OTFyMUKwNlE>
mouse NIH/3T3 cells NV3PbndNTnWwY4Tpc44h[XO|YYm= Mnv3NE4xQC1{MDFOwG0> NXvoZXM4UW6qaXLpeIlwdiCxZjD2MXNz[yCyaH;zdIhwenmuYYTpc44h\XiycnXzd4VlKGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZZQhOC5yODD0c{AzOCC3TTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MYOxPFg1QTl5MR?=

Protocol (from reference)

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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)(C)C

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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