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PP1

Catalog No. T6196 CAS 172889-26-8

Synonyms: EI 275, AGL 1872

PP1 (AGL 1872), a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.

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PP1, CAS 172889-26-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 121.00
25 mg	In stock	$ 212.00
50 mg	In stock	$ 297.00
100 mg	In stock	$ 468.00
500 mg	In stock	$ 1,050.00
1 mL * 10 mM (in DMSO)	In stock	$ 86.00

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Purity: 99.97%

Purity: 99.82%

Purity: 99%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PP1 (AGL 1872), a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
Targets&IC50	Fyn:6 nM, Lck:5 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]
Kinase Assay	Protein A-Sepharose beads (prepared as a 50% (w/v) suspension) are added to the antibody/lysate mixture at 250 μL/mL and allowed to incubate for 30 min at 4°C. The beads are then washed twice in 1 mL of lysis buffer and twice in 1 mL of kinase buffer (25 mM HEPES, 3 mM MnCl2, 5 mM MgCl2, and 100 μM sodium orthovanadate) and resuspended to 50% (w/v) in kinase buffer. Twenty-five microliters of the bead suspension is added to each well of the enolase-coated 96-well high protein binding plate together with an appropriate concentration of compound and [γ-32P]ATP (25 μL/well of a 200 μCi/mL solution in kinase buffer). After incubation for 20 min at 20°C, 60 μL of boiling 2× solubilization buffer containing 10 mM ATP is added to the assay wells to terminate the reactions. Thirty microliters of the samples is removed from the wells, boiled for 5 min, and run on a 7.5% SDS-polyacrylamide gel. The gels are subsequently dried and exposed to Kodak X-AR film. For quantitation, films are scanned using a Molecular Dynamics laser scanner, and the optical density of the major substrate band, enolase p46, is determined. Concentrations of compound that causes 50% inhibition of enolase phosphorylation (IC50) are determined from a plot of the density versus concentration of compound. In companion experiments for measuring the activity of compounds against Lck, the assay plate is washed with two wash cycles on a Skatron harvester using 50 mM EDTA, 1 mM ATP. Scintillation fluid (100 μL) is then added to the wells, and P incorporation is measured using a Pharmacia Biotech micro-β-counter. Concentrations of compound that causes 50% inhibition of enzyme activity (IC50) are determined from a plot of the percent inhibition of enzyme activity versus concentration of compound[1].
Cell Research	PP1 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. Inhibition of anti-CD3-stimulated tyrosine phosphorylation in purified human peripheral blood T cells is measured as follows. All incubations are carried out at 37°C in an Eppendorf Thermomixer 5436 at a mixing setting of 11. Cells (1×106 in 100 μL of RPMI 1640 medium) are incubated for 15 min with drug prior to a 6-min incubation with 1 μg of anti-CD3/mL (anti-leu4, 100 μg/mL). The final volume of the reaction is 115 μL. Reactions are terminated by the addition of 57.5 μL of 3× solubilization buffer incubated at 100°C prior to its addition. Samples are mixed, boiled for 5 min, and stored at -70°C. Western blots of these cell lysates, run on 10% SDS-polyacrylamide gels, are probed with a polyclonal anti-phosphotyrosine antibody, and immune complexes are detected with I-labeled protein A (ICN). For quantitation, films are scanned using a Molecular Dynamics laser scanner, and the optical densities of the major substrate band, p70, are quantitated in the presence of anti-CD3 (in the presence and absence of drug). Percent inhibition is calculated as follows: (1-(p70 optical density units in presence of drug/p70 units in absence of drug))×100. IC50 equals the concentration of compound at which 50% inhibition is measured[1].

Synonyms	EI 275, AGL 1872
Molecular Weight	281.36
Formula	C16H19N5
CAS No.	172889-26-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 4 mg/mL (14.21 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Hanke JH, et al. J Biol Chem, 1996, 271(2), 695-701. 2. Tatton L, et al. J Biol Chem, 2003, 278(7), 4847-4853. 3. Zhao Z, Xue F, Gu Y, et al. Crosstalk between the muscular estrogen receptor α and BDNF/TrkB signaling alleviates metabolic syndrome via 7, 8-dihydroxyflavone in female mice[J]. Molecular Metabolism. 2020: 101149.

Citations

1. Liu X, Yang J, Yang C, et al. Morphine promotes the malignant biological behavior of non-small cell lung cancer cells through the MOR/Src/mTOR pathway. Cancer Cell International. 2021, 21(1): 1-14 2. Zhao Z, Xue F, Gu Y, et al. Crosstalk between the muscular estrogen receptor α and BDNF/TrkB signaling alleviates metabolic syndrome via 7, 8-dihydroxyflavone in female mice. Molecular Metabolism. 2020: 101149. 3. Liu X, Yang J, Yang C, et al. Morphine promotes the malignant biological behavior of non-small cell lung cancer cells through the MOR/Src/mTOR pathway. Cancer cell International. 2021, 21(1): 1-14 4. Liu K, Hao Z, Zheng H, et al.Repurposing of rilpivirine for preventing platelet β3 integrin-dependent thrombosis by targeting c-Src active autophosphorylation.Thrombosis Research.2023 5. Li M Y, Gao R P, Zhu Q, et al.Skeletal muscle-derived FSTL1 starting up angiogenesis by regulating endothelial junction via activating Src pathway can be upregulated by hydrogen sulfide.American Journal of Physiology-Cell Physiology.2023, 325(5): C1252-C1266.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library HIF-1 Signaling Pathway Compound Library Anti-Cancer Compound Library Anti-Liver Cancer Compound Library Cytokine Inhibitor Library Bioactive Compound Library JAK-STAT Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

PP1 172889-26-8 Angiogenesis Apoptosis Cytoskeletal Signaling JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Bcr-Abl Src c-Kit EI 275 AGL1872 EI-275 AGL-1872 PP-1 EI275 AGL 1872 Inhibitor PP 1 inhibit inhibitor

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