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PP1 Src inhibitor

Cat.No.S7060

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

Chemical Structure

Molecular Weight: 281.36

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Quality Control

Batch: Purity: 99.08%
99.08

Cell Culture, Treatment & Working Concentration

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
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
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Solubility

In vitro
Batch:

DMSO : 5 mg/mL (17.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 281.36 Formula

C16H19N5

 Storage (From the date of receipt)
CAS No. 172889-26-8 Download SDF Storage of Stock Solutions

Synonyms AGL 1872, EI 275 Smiles CC1=CC=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)(C)C

Mechanism of Action

Targets/IC50/Ki
LCK
(Cell-free assay)
5 nM
Fyn
(Cell-free assay)
6 nM
Kit
(Cell-free assay)
~75 nM
EGFR
(Cell-free assay)
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. This compound (1 μM) selectively inhibits the induction of the IL-2 gene, but not the granulocyte-macrophage colony-stimulating factor or IL-2 receptor genes. It also inhibits Src (IC50, 170 nM) and Hck (IC50, 20 nM). This chemical is 50–100-fold less active in the inhibition of A-431 epidermal growth factor receptor autophosphorylation (IC50, 0.25 μM). This inhibitor also inhibits Kit and Bcr-Abl tyrosine kinases with IC50 of ∼75 nM and 1 μM, respectively. It completely abrogates the proliferation of M07e cells in response to SCF with IC50 of 0.5–1 μM. This compound (1 μM) inhibits SCF-induced c-Kit autophosphorylation in intact cells and blocks the activation of mitogen-activated protein kinase and Akt. It 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. This chemical 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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