Home Tools

PP2

Catalog No. T6266 CAS 172889-27-9

Synonyms: AGL 1879, AG 1879,AGL 1879

PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PP2, CAS 172889-27-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 63.00
10 mg	In stock	$ 118.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 338.00
100 mg	In stock	$ 536.00
200 mg	In stock	$ 763.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

Bulk Inquiry

Select Batch

Purity: 95.65%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
Targets&IC50	Fyn:5 nM, Lck:4 nM
In vitro	In rats with focal cerebral ischemic damage, PP2 reduces the infarct area by approximately 50%. Compared to the control group, PP2 (1.5 mg/kg, i.p.) significantly improves neurological function scores in rats with this condition. Additionally, in SCID mice implanted with HT29 cells in the spleen, PP2 (5 mg/kg/day) not only decreases the primary tumor growth rate but also significantly reduces relative liver weight and the amount of liver metastasis, compared to the control group.
In vivo	PP2, at concentrations of 1-100 mM, dose-dependently inhibits the growth of the human colon (SW480, HT29, and PMCO1), liver (KYN-2, Li7, PLC/PRF/5, and HepG2), and breast (MDA-MB-468, MCF-7, and BT-474) cancer cells. At 5 µM concentration, PP2 suppresses the phosphorylation and signaling of RET/PTC1 oncoprotein in lysis of NIH3T3 and NIH-RET/PTC3 cells. Additionally, 5 µM PP2 inhibits serum-independent growth in transformed NIH3T3 fibroblasts, and human papillary thyroid carcinoma cell lines TPC1 and FB2 with spontaneous RET/PTC1 rearrangements, as well as hampers Type I collagen matrix invasion by TPC1 cells. At 10 µM, PP2 downregulates the expression levels of pSrc-Y416, pEGFR-Y845, and pEGFR-Y1173 in HeLa and SiHa cells, and regulates cell cycle arrest by upregulating p21(Cip1) and p27(Kip1), and downregulating cyclin A, cyclin-dependent kinases-2 and -4 (Cdk-2, -4) in HeLa cells, and cyclin B and Cdk-2 in SiHa cells. A 20 μM concentration of PP2 inhibits 40-50% of HT29 cell growth within an hour, reduces Src activity maintaining 35% inhibition for two days, and significantly promotes aggregation in most cancer cell lines (HT29, SW480, PMCO1, PLC/PRF/5, KYN-2, Li7, MCF-7, and MDA-MB-468) in an E-cadherin-dependent manner. In cancer cells, 20 μM PP2 boosts E-cadherin expression and its association with the actin cytoskeleton, as well as enhances α-catenin, β-catenin, and γ-catenin expression in HT29 cells, while in PLC/PRF/5 and MCF-7 cells, α-catenin protein levels remain unchanged, and β-catenin and γ-catenin levels slightly increase.
Kinase Assay	Immune complex enzyme assays: The acid-treated enolase is diluted 1:20 with 1&times 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&times PBS for 1 h at 37 ℃;and then washed five times with 300 mL of 1&times 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&times 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, 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 ℃, 60 μLl of boiling 2&times 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	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)

Synonyms	AGL 1879, AG 1879,AGL 1879
Molecular Weight	301.77
Formula	C15H16ClN5
CAS No.	172889-27-9

Storage

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

Solubility Information

DMSO: 56 mg/mL (185.6 mM)

Ethanol: 2 mg/mL (6.62 mM)

References and Literature

1. Hanke JH, et al. J Biol Chem, 1996, 271(2), 695-701. 2. Karni R, et al. FEBS Lett, 2003, 537(1-3), 47-52. 3. Nam JS, et al. Clin Cancer Res, 2002, 8(7), 2430-2436. 4. Kong L, et al. Mol Cell Biochem, 2011, 348(1-2), 11-19. 5. Lennmyr F, et al. Acta Neurol Scand, 2004, 110(3), 175-179. 6. Inoue A, et al. Phosphorylation of NMDA receptor GluN2B subunit at Tyr1472 is important for trigeminal processing of itch. Eur J Neurosci. 2016 Oct;44(7):2474-2482.

Citations

1. Zheng T, Wang H Y, Chen Y, et al. Src Activation Aggravates Podocyte Injury in Diabetic Nephropathy via Suppression of FUNDC1-Mediated Mitophagy. Frontiers in Pharmacology. 2022, 13: 897046-897046 2. 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

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Inhibitor Library Kinase Inhibitor Library Apoptosis Compound Library Anti-Breast Cancer Compound Library Epigenetics Compound Library Cytokine Inhibitor Library HIF-1 Signaling Pathway Compound Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets

PF-6274484 2′-Thioadenosine Mutated EGFR-IN-1 Olmutinib Lidocaine Hydrochloride hydrate AG1557 Panitumumab Nazartinib

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PP2 172889-27-9 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK EGFR Src AGL 1879 AG 1879,AGL-1879 AG 1879,AGL 1879 AGL-1879 Inhibitor AGL1879 inhibit PP-2 AG 1879,AGL1879 PP 2 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.