Home Angiogenesis Src inhibitor PP1 For research use only.

PP1

Synonyms: AGL 1872, EI 275

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

PP1 Chemical Structure

CAS No. 172889-26-8

Purity & Quality Control

PP1 Related Products

Signaling Pathway

Src Signaling Pathways

Src Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat cells Function assay Inhibition of MLR stimulated IL-2 production in Jurkat cells, IC50=0.4 μM 11012021
mouse NIH/3T3 cells Function assay 0.08-20 μM Inhibition of v-Src phosphorylation expressed in mouse NIH/3T3 cells at 0.08 to 20 uM by Western blot analysis 18849971
Click to View More Cell Line Experimental Data

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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00791843 Completed
Congestive Heart Failure
University of Pennsylvania
 March 2004 Phase 2

Chemical Information & Solubility

Molecular Weight 281.36 Formula

C16H19N5
CAS No. 172889-26-8 SDF Download PP1 SDF
Smiles CC1=CC=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 5 mg/mL ( (17.77 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

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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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