PP2

Catalog No.S7008 Synonyms: AG 1879,AGL 1879

PP2 Chemical Structure

Molecular Weight(MW): 301.77

PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.

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In DMSO USD 180 In stock
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Cited by 24 Publications

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Biological Activity

Description PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.
Targets
LCK [1]
(Cell-free assay)
Fyn [1]
(Cell-free assay)
4 nM 5 nM
In vitro

PP2 inhibits Src by binding to an area of the molecule that does not overlap with the ATP binding domain. [2] PP2 (20 μM) induces 40-50% growth inhibition of HT29 cells, this concentration reduces the Src activity as early as 1 hour and maintains a 35% inhibition of Src activity for 2 days. PP2 (100 mM) decreases the Src activity of HT29 cells in a dose-dependent manner. PP2 (1 mM-100 mM) causes a dose-dependent growth inhibition of human colon cancer cells (HT29, SW480, and PMCO1), liver cancer cells (PLC/PRF/5, KYN-2, Li7, and HepG2), and breast cancer cells (MCF-7, MDA-MB-468, and BT-474). PP2 (20 μM) significantly increases aggregation in most of the cancer cells (HT29, SW480, PMCO1, PLC/PRF/5, KYN-2, Li7, MCF-7, and MDA-MB-468) in E-cadherin dependent manner. PP2 (20 μM) enhances E-cadherin expression and also strongly increases E-cadherin’s association with the actin cytoskeleton in cancer cells. PP2 (20 μM) increases the expression of α-catenin, β-catenin, and γ-catenin in HT29 cells, whereas in PLC/PRF/5 and MCF-7 cells, the total protein level of α-catenin does not change, but the levels of β- catenin and γ-catenin increases slightly. [3] PP2 inhibits proliferation of two cervical cancer cells (HeLa and SiHa) in a time- and dose-dependent manner. PP2 (10 μM) down-regulates pSrc-Y416, pEGFR-Y845, and -Y1173 expression levels in HeLa and SiHa cells. PP2 (10 μM) could modulate cell cycle arrest by up-regulating p21(Cip1) and p27(Kip1) in both HeLa and SiHa cells and down-regulating expression of cyclin A, and cyclin dependent kinase-2, -4 (Cdk-2, -4) in HeLa and of cyclin B and Cdk-2 in SiHa. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human T cells NFPic|BHfW6ldHnvckBie3OjeR?= NWrJUWM2UW6qaXLpeIlwdiCxZjDh[Ihme2mxbjDrbY5ie2ViaX6gbJVu[W5iVDDj[YxteyxiSVO1NF0xNjZizszNMi=> NGLuTpYyQDB5N{O2Ny=>
human T cells MYHGeY5kfGmxbjDhd5NigQ>? M2XWPGlvcGmkaYTpc44hd2ZidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFRiY3XscJMtKEmFNUC9NE43KM7:TT6= NUP3ZohrOThyN{ezOlM>
human Saos2 cells MYPDfZRwfG:6aXRCpIF{e2G7 M2[wRVQ5KGh? MnWwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV4FwezJiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME24MlA4KM7:TR?= MnjwNlM6OzJyN{C=
human SaOS2 cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 Mly5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVYV;TNkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyudXzhdkB3cWGkaXzpeJktKEmFNUC9PE4yKM7:TR?= NGTUd5cyPzl{OUe5Ni=>
human MEG01 cells NYTsdmM1WHKxbHnm[ZJifGmxbjDhd5NigQ>? MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2HR{CxJINmdGy|LDDJR|UxRTF5IN88US=> Mn:2NVgzPTd3MUO=
A431 cells NUW4O4VKTnWwY4Tpc44h[XO|YYm= NEDQcWtKdmirYnn0c5J6KGWoZnXjeEBwdiCyaH;zdIhwNVO{Yz;uc45xcG:|cHjvJIFnfGW{IFXHSkApOTByIIXNLUB{fGmvdXzheIlwdiCxZjDBOFMyKGOnbHzzMEBKSzVyPUG3JO69VQ>? M4rycVE2OTB7NkSy
human K562 cells MonRVJJwdGmoZYLheIlwdiCjc4PhfS=> M1nifWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczygTWM2OD1{NTFOwG0> M3\4SFE5OjV5NUGz
human KU812 cells NVfyUYtSWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4LRZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS2W4NVIh[2WubIOsJGlEPTB;NEWg{txO NXXDOmtJOTh{NUe1NVM>
8701-BC cells NVvCOGxWTnWwY4Tpc44h[XO|YYm= NHqyd4EyOCEQvF2= NFXucmFRem:jcH;weI91cWNiYXP0bZZqfHliYXfhbY5{fCB6N{CxMWJEKGOnbHzzJIF1KDFyIIXNJIJ6KFCDUmCgZZN{[Xl? M2TwR|E3PTB7NUez
A431 cells M2TI[GZ2dmO2aX;uJIF{e2G7 NG[xXG0yOCEQvF2= NFfMfYFKdmirYnn0bY9vKG:oIGPyZ{BifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIGm0NVkhcW5iQUSzNUBk\WyuczDheEAyOCC3TR?= NX7Rcld7OTZ3MEm1O|M>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-PI3K / PI3K / p-AKT / AKT / Bcl-2 / Caspase-3 ; 

PubMed: 30250573     


Protein expression of the PI3K/Akt/Bcl-2/caspase-3 signaling pathway members in A549 cells treated with various concentrations of PP2.

p-Src / Src / p-MAPK / MAPK ; 

PubMed: 23704208     


MCF-7:5C cells were treated with vehicle (0.1% DMSO) and PP2 (5×10−6mol/L) for different durations. Phosphorylated c-Src, MAPK, and Akt were detected by immunoblotting. Total c-Src, MAPK, and Akt were used for loading controls. 

30250573 23704208
Immunofluorescence
β-catenin; 

PubMed: 18566211     


Immunofluorescence staining of β-catenin (green) of PP2 and vehicle-treated PC3 cells. Propidium iodide stains the nucleus (red). Bar represents 15 μm.

FAK / p-FAK ; 

PubMed: 17927818     


PP2 promotes cell rounding and cortical actin formation. Primary mouse chondrocytes were incubated for 24 hours with dimethyl sulphoxide (DMSO) or the Src inhibitor PP2 (10 μmol/l), and cells were stained with antibodies against total focal adhesion kinase (FAK) or FAK phosphorylated on residue tyrosine 397 (green), rhodamine-phalloidin (red) and DAPI (blue). In the presence of DMSO, total and phosphorylated actin localized to focal adhesions at the end of stress fibres. In cells treated with PP2, total FAK acquired a diffuse cytosolic staining, whereas the signal for phosphorylated FAK was greatly reduced (scale bar: 2 μm).

18566211 17927818
In vivo PP2 (5 mg/kg/day) induces some slowing in the growth rate of the primary tumors relative to the control treated with vehicle in SCID mice inoculated HT29 cells in the spleen. PP2 (5 mg/kg/day) induces some slowing in the growth rate of the primary tumors relative to the control treated with vehicle in SCID mice inoculated HT29 cells in the spleen. PP2 (5 mg/kg/day) significantly reduces the relative liver weight and liver metastasis volume compared with the controls in SCID mice inoculated HT29 cells in the spleen. [3] PP2 (1.5 mg/kg i.p.) treated rats show approximately 50% reduction of infarct size on T2-weighted MRI and in TTC staining compared with controls in rats with focal ischemic brain injury. PP2 (1.5 mg/kg i.p.) results in better the neurological score than controls in rats with focal ischemic brain injury. [5]

Protocol

Kinase Assay:[1]
+ Expand

Immune complex enzyme assays:

The acid-treated enolase is diluted 1:20 with 1× PBS before aliquoting 100 mL/well into a Nunc 96-well high protein binding assay plate. Assay wells are then aspirated; blocked with 0.5% bovine serum, 1× PBS for 1 h at 37 ℃;and then washed five times with 300 mL of 1× PBS/well. The source of Lck is either LSTRA cells or Lck expressed in HeLa cells using a vaccinia expression system. FynT is expressed in HeLa cells using the vaccinia system. Cells (12.5× 106/mL) are lysed in lysis buffer (20 mM Tris, pH 8.0, 150 mM NaCl, 0.5% Nonidet P-40, and 23 trypsin inhibitory units/mL aprotinin), and the lysates are clarified by centrifugation at 14,000 cpm for 15 min at 4 ℃ in an Eppendorf tube. The clarified lysates are then incubated with the appropriate anti-kinase antibody at 10 μg/mL for 2 h at 4 ℃. Protein A-Sepharose beads are added to the antibody/lysate mixture at 250 μL/mL and allowed to incubate for 30 min at 4 ℃. 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, 5mM 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 ℃, 60 μLl 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. 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 32P incorporation is measured using a micro-β-counter.
Cell Research:[3]
+ Expand
  • Cell lines: HT29, SW480, PMCO1, PLC/PRF/5, KYN-2, Li7, HepG2, MCF-7, MDA-MB-468 and BT-474 cell lines
  • Concentrations: ~100 μM
  • Incubation Time: 2 days
  • Method: Cell viability is determined using an in vitro toxicology assay kit following the manufacturer’s instructions. Cells are seeded in 96-well plates at day 0. Starting at day 1, cells are treated for 2 days with each of a series of increasing concentrations of PP2 (1 μM, 10 μM, and 100 μM). At the end of this period, cell proliferation is evaluated by a colorimetric assay based on the cleavage of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide by mitochondria dehydrogenase in viable cells, leading to formazan formation. This experiment is repeated three times with 10 determinations/tested concentration.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: SCID mice inoculated HT29 cells in the spleen
  • Formulation: 1% DMSO
  • Dosages: 5 mg/kg/day
  • Administration: intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (198.82 mM)
Ethanol 2 mg/mL (6.62 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.
2.5mg/mL

* 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 301.77
Formula

C15H16ClN5

CAS No. 172889-27-9
Storage powder
in solvent
Synonyms AG 1879,AGL 1879

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03842371 Not yet recruiting Other: Metabolic level of BCAAs in monocytes and macrophages Sepsis Syndrome West China Hospital February 11 2019 --
NCT02407626 Terminated Drug: Propofol|Drug: Sevoflurane Myocardial Ischemia Triemli Hospital|University of Alberta September 2015 Not Applicable
NCT02315287 Recruiting Drug: Pioglitazone|Drug: Lobeglitazone Type 2 Diabetes Seoul National University Bundang Hospital September 2014 Phase 4
NCT02036554 Unknown status Drug: Everolimus|Drug: Tacrolimus|Drug: Mycophenolic acid Kidney; Complications Allograft Seoul St. Mary''s Hospital|Novartis March 2013 Phase 4

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Frequently Asked Questions

  • Question 1:

    Could you please suggest me the in vivo details about the dilution to reduce the amount of DMSO to 1 to 5%?

  • Answer:

    For in vivo study, we recommend to use 4% DMSO +Corn oil up to 2.5 mg/ml.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID