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PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
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PP2 Chemical Structure
CAS No. : 172889-27-9
This product is a controlled substance and not for sale in your territory.
Based on 46 publication(s) in Google Scholar
PP2 purchased from MedChemExpress. Usage Cited in:
FASEB J. 2020 Aug;34(8):10443-10461.
[Abstract]
Cells are pretreated with PP2 (10 μM) for 24 hours and further treated with MMS, and GAPDH nuclear translocation is visualized by confocal microscopy. The immunofluorescence staining results directly show that inhibiting Src activity by PP2 decreases GAPDH nuclear distribution in response to MMS.
PP2 purchased from MedChemExpress. Usage Cited in:
Cancer Sci. 2018 May;109(5):1648-1659.
[Abstract]
Cells are treated with vehicle (0.1% DMSO) or PP2 (2.5 μM and 5 μM) for 48 h. Cell lysates are harvested. Total and phosphorylated c-Src are detected by western blotting.
PP2 purchased from MedChemExpress. Usage Cited in:
J Cell Mol Med. 2018 May 12;22(8):3768-3781.
[Abstract]
Prostate cancer cells are grown and treated with different concentrations of the Src inhibitor PP2 for 2 h and subjected to Western blot analysis. The data show that the inhibition of Src dose dependently decreases levels of p-Src527 but not p-Src426.
PP2 purchased from MedChemExpress. Usage Cited in:
Oncotarget. 2017 Nov 22;8(65):109135-109150.
[Abstract]
MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.
PP2 purchased from MedChemExpress. Usage Cited in:
Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2015 Jul;27(7):568-73.
[Abstract]
To determine whether the inhibition of caveolin-1 tyrosine residues 14 ( Cav-1-Y14 ) phosphorylation with protein tyrosine kinase inhibitors ( PP2 ) will upregulate heme oxygenase-1 ( HO-1 ) activity to protect against ventilation induced lung injury in vivo of an animal model. The group D1 or D2 receive high tidal volume ventilation for 1 hour or 2 hour respectively, but they are given PP2 1 hour before high tidal volume ventilation. The groups E1 and E2 also receive high tidal volume ventilat
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Lck Fyn Blk
Description
PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
IC50 & Target
IC50: 4 nM (Lck), 5 nM (Fyn)[1]
Cellular Effect
Cell Line
Type
Value
Description
References
8701-BC
IC50
61.8 μM
Compound: PP2
In vitro antiproliferative activity against 8701-BC human breast cancer cells at a concentration of (0-100 uM) for 72 hr using MTT assay
In vitro antiproliferative activity against 8701-BC human breast cancer cells at a concentration of (0-100 uM) for 72 hr using MTT assay
[PMID: 15027847]
SAOS-2
IC50
8.07 μM
Compound: PP2
Cytotoxicity against human Saos2 cells after 48 hrs by MTT assay
Cytotoxicity against human Saos2 cells after 48 hrs by MTT assay
[PMID: 23932070]
SH-SY5Y
IC50
6.1 μM
Compound: PP2
Antiproliferative activity against human SH-SY5Y cells assessed as cell viability after 72 hrs by XTT assay
Antiproliferative activity against human SH-SY5Y cells assessed as cell viability after 72 hrs by XTT assay
[PMID: 21856155]
In Vitro
At 10 μM, the effect of PP2 on cellular proliferation is not significant, indicating that, at this low concentration, the effect of PP2 on Gemcitabine cytotoxicity does not simply reflect a direct antiproliferative effect, but rather a potentiation of Gemcitabine-induced cytotoxicity. Above 20 μM, growth is increasingly suppressed, a finding consistent with reports in other human cancer cell lines. Although 10 μM PP2 is used in our study, at higher concentrations PP2 is reported to inhibit other intracellular kinases[2]. PP2 is the most widely used commercially available Src family kinase inhibitor. PP2 inhibits Src family kinase activity with IC50 of ~5 nM in vitro, concentrations to 10 μM are often necessary to achieve complete Src family kinase inhibition in cell culture[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PP2 Related Antibodies
In Vivo
The tumor growth inhibition rate is 25% in the PP2 treatment group and 5% in the Gemcitabine treatment group (P>0.05). When administered in combination, PP2 and Gemcitabine produce a tumor growth inhibition rate of 98% (P<0.05). Hepatic metastasis occurred in 100% of control and Gemcitabine-treated groups; 88% of the PP2-treated group developed liver metastases. There are no detectable metastases in the group treated with PP2 and Gemcitabine in combination (P<0.05)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Masse moléculaire
301.77
Formule
C15H16ClN5
CAS No.
172889-27-9
Appearance
Solid
Color
White to off-white
SMILES
NC1=C2C(N(C(C)(C)C)N=C2C3=CC=C(Cl)C=C3)=NC=N1
Livraison
Room temperature in continental US; may vary elsewhere.
Stockage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (165.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
3.3138 mL
16.5689 mL
33.1378 mL
5 mM
0.6628 mL
3.3138 mL
6.6276 mL
10 mM
0.3314 mL
1.6569 mL
3.3138 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (9.94 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (30.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Hanke JH, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck-and FynT-dependentT cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701.
[Content Brief]
[2]. Duxbury MS, et al. Inhibition of SRC tyrosine kinase impairs inherent and acquired Gemcitabine resistance in human pancreatic adenocarcinoma cells. Clin Cancer Res. 2004 Apr 1;10(7):2307-18
[Content Brief]
[3]. Summy JM, et al. AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Mol Cancer Ther. 2005 D
[Content Brief]
[4]. 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.
[Content Brief]
Test cellulaire
[2]
Cell growth is determined by MTT assay and confirmed by cell counting. Results of the MTT assay have been shown to correlate well with [3H]thymidine incorporation in pancreatic cancer cell lines. Logarithmically growing cells are plated at 5×103 cells/well in 96-well plates, allowed to adhere for 24 h, and cultured in the presence or absence of PP2 and Gemcitabine. Cell proliferation is determined after 96 h. Plates are read using a Vmax microplate spectrophotometer at a wavelength of 570 nm corrected to 650 nm and normalized to controls. Each independent experiment is performed three times, with 10 determinations for each condition tested. The IC50 of Gemcitabine is calculated from these results. At identical time points, cells are trypsinized to form a single cell suspension. Intact cells, determined by trypan blue exclusion, are counted using a Neubauer hemocytometer, and the number of cells per mL is calculated and compared with the control group to confirm the MTT results[2].
MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale
[2]
Mice[2] Male athymic nu/nu mice (age, 5 weeks; weight, 20-22 g; specific pathogen free) are anesthetized with i.p. ketamine (200 mg/kg) and xylazine (10 mg/kg) and inoculated with 106 Gemcitabine-resistant PANC1GemRes cells in 20 μL of PBS by surgical orthotopic implantation into the pancreas. After inoculation, mice are randomized to three treatment groups: (a) treatment group 1 (n=8) receive 2 mg/kg PP2 in 1% DMSO by i.p. injection three times a week; (b) treatment group 2 (n=8) receive Gemcitabine (100 mg/kg) in the same volume of 1% DMSO vehicle as received by group 1, three times a week; and (c) treatment group 3 (n=8) receive 2 mg/kg PP2 and 100 mg/kg Gemcitabine in the same volume of DMSO as groups 1 and 2, three times a week. The control group receive the same volume of 1% DMSO vehicle as the other groups, three times a week. Treatment is commenced 1 day after implantation, and necropsy is performed 4 weeks after implantation. Primary tumors are identified, weighed, and normalized to total body mass. Tumor growth inhibition rate is calculated using the following formula: tumor growth inhibition rate (%)=(1−MT/MC)×100, where MT and MC are the mean normalized tumor masses of treatment and control groups, respectively. Liver metastases are counted and confirmed histologically.
MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références
[1]. Hanke JH, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck-and FynT-dependentT cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701.
[Content Brief]
[2]. Duxbury MS, et al. Inhibition of SRC tyrosine kinase impairs inherent and acquired Gemcitabine resistance in human pancreatic adenocarcinoma cells. Clin Cancer Res. 2004 Apr 1;10(7):2307-18
[Content Brief]
[3]. Summy JM, et al. AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Mol Cancer Ther. 2005 D
[Content Brief]
[4]. 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.
[Content Brief]
[1]. Hanke JH, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck-and FynT-dependentT cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701.
[2]. Duxbury MS, et al. Inhibition of SRC tyrosine kinase impairs inherent and acquired Gemcitabine resistance in human pancreatic adenocarcinoma cells. Clin Cancer Res. 2004 Apr 1;10(7):2307-18
[3]. Summy JM, et al. AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Mol Cancer Ther. 2005 D
[4]. 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.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
3.3138 mL
16.5689 mL
33.1378 mL
82.8446 mL
5 mM
0.6628 mL
3.3138 mL
6.6276 mL
16.5689 mL
10 mM
0.3314 mL
1.6569 mL
3.3138 mL
8.2845 mL
15 mM
0.2209 mL
1.1046 mL
2.2092 mL
5.5230 mL
20 mM
0.1657 mL
0.8284 mL
1.6569 mL
4.1422 mL
25 mM
0.1326 mL
0.6628 mL
1.3255 mL
3.3138 mL
30 mM
0.1105 mL
0.5523 mL
1.1046 mL
2.7615 mL
40 mM
0.0828 mL
0.4142 mL
0.8284 mL
2.0711 mL
50 mM
0.0663 mL
0.3314 mL
0.6628 mL
1.6569 mL
60 mM
0.0552 mL
0.2761 mL
0.5523 mL
1.3807 mL
80 mM
0.0414 mL
0.2071 mL
0.4142 mL
1.0356 mL
100 mM
0.0331 mL
0.1657 mL
0.3314 mL
0.8284 mL
PP2 Related Classifications
Protein Tyrosine Kinase/RTK
Src
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Telefono : +1 850 650 7790