PP2
Based on 64 publication(s) in Google Scholar
PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
For research use only. We do not sell to patients.
- Purity: 99.14%
- CAS No.: 172889-27-9
- Formula: C15H16ClN5
- Molecular Weight:301.77
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) PP2
More- Signal Transduct Target Ther. 2023 Feb 17;8(1):66. [Abstract]
- Cancer Cell. 2024 Apr 8;42(4):682-700.e12. [Abstract]
- Nat Immunol. 2023 Nov;24(11):1813-1824. [Abstract]
- Cell Stem Cell. 2022 Jul 7;29(7):1119-1134.e7. [Abstract]
- Nat Commun. 2025 May 8;16(1):4288. [Abstract]
- Nat Commun. 2024 Aug 28;15(1):7455. [Abstract]
- Nat Commun. 2020 Sep 21;11(1):4765. [Abstract]
- ACS Nano. 2021 Sep 28;15(9):14360-14372. [Abstract]
- Sci Immunol. 2025 Jun 27;10(108):eadn1630. [Abstract]
- Sci Immunol. 2022 Jan 21;7(67):eabj5501. [Abstract]
- Genes Dis. 2025 Nov 6.
- J Exp Clin Cancer Res. 2022 Apr 5;41(1):125. [Abstract]
- Sci Adv. 2025 Nov 28;11(48):eadz2345. [Abstract]
- Carbohydr Polym. 2026 Feb 15:374:124706. [Abstract]
- Carbohydr Polym. 2023 Oct 1:317:121108. [Abstract]
- Cell Death Dis. 2022 Feb 17;13(2):158. [Abstract]
- Cell Death Dis. 2021 Dec 3;12(12):1126. [Abstract]
- Phytomedicine. 2025 Dec:149:157553. [Abstract]
- Food Chem. 2021 Nov 30:363:130323. [Abstract]
- Int J Surg. 2025 Nov 10. [Abstract]
- Int J Biol Macromol. 2026 Feb:347:150757. [Abstract]
- J Headache Pain. 2022 Aug 10;23(1):98. [Abstract]
- Neural Regen Res. 2025 Apr 29. [Abstract]
- Cell Rep. 2023 Mar 30;42(4):112314. [Abstract]
- Cell Rep. 2020 Mar 24;30(12):4235-4249.e6. [Abstract]
- Fundam Res. 2024 Apr 15.
- J Ethnopharmacol. 2020 May 23:254:112723. [Abstract]
- Mech Ageing Dev. 2026 Jan 15:230:112156. [Abstract]
- Biochem Pharmacol. 2022 Dec:206:115339. [Abstract]
- Life Sci. 2022 Apr 15:295:120419. [Abstract]
- Life Sci. 2019 Mar 15:221:35-46. [Abstract]
- Life Metab. 2025 Jan 29;4(2):loaf002. [Abstract]
- Bioeng Transl Med. 2023 Oct 7;9(1):e10603. [Abstract]
- EMBO Rep. 2023 Aug 3;24(8):e56437. [Abstract]
- Cells. 2020 Jun 15;9(6):1467. [Abstract]
- Cells. 2020 Mar 5;9(3):631. [Abstract]
- mBio. 2026 Apr 8;17(4):e0389625. [Abstract]
- Chem Biol Interact. 2025 Jan 5:405:111269. [Abstract]
- mSystems. 2020 Jun 2;5(3):e00176-20. [Abstract]
- PLoS Pathog. 2024 Oct 29;20(10):e1012674. [Abstract]
- Cancer Sci. 2018 May;109(5):1648-1659. [Abstract]
- J Cell Mol Med. 2018 Aug;22(8):3768-3781. [Abstract]
- FASEB J. 2020 Aug;34(8):10443-10461. [Abstract]
- J Virol. 2023 Mar 30;97(3):e0154522. [Abstract]
- Nanotoxicology. 2026 May 19:1-18. [Abstract]
- Reprod Toxicol. 2025 Sep 8:109047. [Abstract]
- FEBS Lett. 2020 Jul;594(14):2294-2302. [Abstract]
- Steroids. 2021 Nov:175:108915. [Abstract]
- Eur J Neurosci. 2016 Oct;44(7):2474-2482. [Abstract]
- J Biochem. 2022 Mar 3;171(3):349-359. [Abstract]
- Neurol Res. 2025 Sep;47(9):864-875. [Abstract]
- Reprod Dev Med. October 27, 2022.
- Res Sq. 2026 May 19.
- Jagiellonian University. 2026.
- Technical University of Dresden. 2025.
- University of Toronto. 2026.
- bioRxiv. 2025 Oct 24.
- bioRxiv. 2025 Jun 16:2025.06.11.659120. [Abstract]
- bioRxiv. 2025 Jun 21.
- Research Square Preprint. 2024 Jan 1.
- Research Square Preprint. 2024 Jan 25.
- Bioengineered. 2021 Dec;12(2):11390-11398. [Abstract]
- Oncotarget. 2017 Nov 22;8(65):109135-109150. [Abstract]
- Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2015 Jul;27(7):568-73. [Abstract]
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IF
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WB
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WB
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WB
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WB
Biological Activity
IC50: 4 nM (Lck), 5 nM (Fyn)[1]
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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] |
| 8701-BC | IC50 |
61.8 μM
Compound: PP2
|
Antiproliferative activity against 8701-BC cells
Antiproliferative activity against 8701-BC cells
|
[PMID: 16509573] |
| A-431 | IC50 |
131 μM
Compound: PP2
|
Inhibitory effect on nonphospho-Src after EGF (100 uM) stimulation of A431 cells (control=178)
Inhibitory effect on nonphospho-Src after EGF (100 uM) stimulation of A431 cells (control=178)
|
[PMID: 15109642] |
| A-431 | IC50 |
17 μM
Compound: PP2
|
Inhibitory effect on phospho-Src/nonphospho after EGF (100 uM) stimulation of A431 cells (21)
Inhibitory effect on phospho-Src/nonphospho after EGF (100 uM) stimulation of A431 cells (21)
|
[PMID: 15109642] |
| A-431 | IC50 |
22 μM
Compound: PP2
|
Inhibitory effect on phospho-Src (Tyr416) after EGF (100 uM) stimulation of A431 cells (38)
Inhibitory effect on phospho-Src (Tyr416) after EGF (100 uM) stimulation of A431 cells (38)
|
[PMID: 15109642] |
| A-431 | IC50 |
32 μM
Compound: PP2
|
Tested for antiproliferative activity against human A431 cells
Tested for antiproliferative activity against human A431 cells
|
[PMID: 15109642] |
| A-431 | IC50 |
32.2 μM
Compound: PP2
|
Antiproliferative activity against A431 cells
Antiproliferative activity against A431 cells
|
[PMID: 16509573] |
| A549 | IC50 |
0.01 μM
Compound: PP2
|
Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
|
[PMID: 28814374] |
| Jurkat | IC50 |
4 nM
Compound: PP2
|
Inhibition of p56 Lck tyrosine kinase in Jurkat cells where p56lck autophosphorylation is inhibited.
Inhibition of p56 Lck tyrosine kinase in Jurkat cells where p56lck autophosphorylation is inhibited.
|
10.1016/S0960-894X(97)00034-6 |
| K562 | IC50 |
25 μM
Compound: 8, PP2
|
Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
|
[PMID: 18257513] |
| KU812 cell line | IC50 |
45 μM
Compound: 8, PP2
|
Antiproliferative activity against human KU812 cells
Antiproliferative activity against human KU812 cells
|
[PMID: 18257513] |
| MEG-01 | IC50 |
17 μM
Compound: 8, PP2
|
Antiproliferative activity against human MEG01 cells
Antiproliferative activity against human MEG01 cells
|
[PMID: 18257513] |
| 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
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[PMID: 23932070] |
| SAOS-2 | IC50 |
8.1 μM
Compound: PP2
|
Antiproliferative activity against human SaOS2 cells assessed as cellular viability
Antiproliferative activity against human SaOS2 cells assessed as cellular viability
|
[PMID: 17929792] |
| 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] |
| T-cell | IC50 |
600 nM
Compound: K00048, AG-1879
|
Inhibition of adhesion kinase in human T cells
Inhibition of adhesion kinase in human T cells
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[PMID: 18077363] |
| T-cell | IC50 |
600 nM
Compound: K00048, AG-1879
|
Inhibition of tyrosine phosphorylation in human T cells
Inhibition of tyrosine phosphorylation in human T cells
|
[PMID: 18077363] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 172889-27-9
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Appearance Solid
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Molecular Weight 301.77
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Formula C15H16ClN5
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Color White to off-white
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SMILES
NC1=C2C(N(C(C)(C)C)N=C2C3=CC=C(Cl)C=C3)=NC=N1
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Synonyms
AGL 1879
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (64)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
B-lymphoid tyrosine kinase-mediated FAM83A phosphorylation elevates pancreatic tumorigenesis through interacting with β-catenin. [Abstract]2023 Feb 17;8(1):66. PMID: 36797256 -
Cancer Cell
PDGFRα+ITGA11+ fibroblasts foster early-stage cancer lymphovascular invasion and lymphatic metastasis via ITGA11-SELE interplay. [Abstract]2024 Apr 8;42(4):682-700.e12. PMID: 38428409 -
Nat Immunol
The ligation between ERMAP, galectin-9 and dectin-2 promotes Kupffer cell phagocytosis and antitumor immunity. [Abstract]2023 Nov;24(11):1813-1824. PMID: 37813965 -
Cell Stem Cell
Amino acid catabolism regulates hematopoietic stem cell proteostasis via a GCN2-eIF2α axis. [Abstract]2022 Jul 7;29(7):1119-1134.e7. PMID: 35803229 -
Nat Commun
Structure-based design of potent and selective inhibitors targeting RIPK3 for eliminating on-target toxicity in vitro. [Abstract]2025 May 8;16(1):4288. PMID: 40341069 -
Nat Commun
The proto-oncogene tyrosine kinase c-SRC facilitates glioblastoma progression by remodeling fatty acid synthesis. [Abstract]2024 Aug 28;15(1):7455. PMID: 39198451 -
Nat Commun
2020 Sep 21;11(1):4765. PMID: 32958780 -
ACS Nano
Apoptotic Extracellular Vesicles Ameliorate Multiple Myeloma by Restoring Fas-Mediated Apoptosis. [Abstract]2021 Sep 28;15(9):14360-14372. PMID: 34506129 -
Sci Immunol
Radiotherapy enhances anticancer CD8 T cell responses by cGAMP transfer through LRRC8A/C volume-regulated anion channels. [Abstract]2025 Jun 27;10(108):eadn1630. PMID: 40577443 -
Sci Immunol
SLAMF3 and SLAMF4 are immune checkpoints that constrain macrophage phagocytosis of hematopoietic tumors. [Abstract]2022 Jan 21;7(67):eabj5501. PMID: 35061505 -
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J Exp Clin Cancer Res
PPFIA4 promotes castration-resistant prostate cancer by enhancing mitochondrial metabolism through MTHFD2. [Abstract]2022 Apr 5;41(1):125. PMID: 35382861 -
Sci Adv
FeaSion decodes the regulatory landscape and functional diversity of RNA polymerase II CTD phosphorylation. [Abstract]2025 Nov 28;11(48):eadz2345. PMID: 41313762 -
Carbohydr Polym
Decoding the pharmacokinetics of intravenous lentinan: A multiscale journey from the blood to hepatic Kupffer cells' lysosomes. [Abstract]2026 Feb 15:374:124706. PMID: 41371850 -
Carbohydr Polym
Metabolic degradation of polysaccharides from Lentinus edodes by Kupffer cells via the Dectin-1/Syk signaling pathway. [Abstract]2023 Oct 1:317:121108. PMID: 37364942 -
Cell Death Dis
Targeting CCL2-CCR4 axis suppress cell migration of head and neck squamous cell carcinoma. [Abstract]2022 Feb 17;13(2):158. PMID: 35177591 -
Cell Death Dis
Hippo signaling suppresses tumor cell metastasis via a Yki-Src42A positive feedback loop. [Abstract]2021 Dec 3;12(12):1126. PMID: 34862372 -
Phytomedicine
Liquiritigenin attenuates thrombosis by inhibiting P2Y12R-mediated Src/PLCγ2 signaling and cytoplasmic Ca2+ mobilization in platelets. [Abstract]2025 Dec:149:157553. PMID: 41273866 -
Food Chem
Ex vivo to in vivo extrapolation of syringic acid and ferulic acid as grape juice proxies for endothelium-dependent vasodilation: Redefining vasoprotective resveratrol of the French paradox. [Abstract]2021 Nov 30:363:130323. PMID: 34247035 -
Int J Surg
C-Src/β-DG-mediated impairment of glia-vascular unit integrity via AQP4 depolarization contributes to secondary hydrocephalus after intraventricular hemorrhage. [Abstract]2025 Nov 10. PMID: 41208590 -
Int J Biol Macromol
Omentin-1 promotes diabetic wound healing by regulating macrophage efferocytosis and M2 polarization. [Abstract]2026 Feb:347:150757. PMID: 41654047 -
J Headache Pain
Dopamine receptor D2 regulates GLUA1-containing AMPA receptor trafficking and central sensitization through the PI3K signaling pathway in a male rat model of chronic migraine. [Abstract]2022 Aug 10;23(1):98. PMID: 35948867 -
Neural Regen Res
5-O-Methylvisammioside alleviates depression-like behaviors by inhibiting nuclear factor kappa B pathway activation via targeting SRC. [Abstract]2025 Apr 29. PMID: 40313111 -
Cell Rep
2023 Mar 30;42(4):112314. PMID: 37000627 -
Cell Rep
2020 Mar 24;30(12):4235-4249.e6. PMID: 32209481 -
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J Ethnopharmacol
A peptide inhibitor of macrophage migration in atherosclerosis purified from the leech Whitmania pigra. [Abstract]2020 May 23:254:112723. PMID: 32119950 -
Mech Ageing Dev
2026 Jan 15:230:112156. PMID: 41547434 -
Biochem Pharmacol
The ubiquitination of CKIP-1 mediated by Src aggravates diabetic renal fibrosis (original article). [Abstract]2022 Dec:206:115339. PMID: 36347273 -
Life Sci
EphrinB2/ephB2 activation facilitates colonic synaptic potentiation and plasticity contributing to long-term visceral hypersensitivity in irritable bowel syndrome. [Abstract]2022 Apr 15:295:120419. PMID: 35183555 -
Life Sci
Panaxadiol inhibits synaptic dysfunction in Alzheimer's disease and targets the Fyn protein in APP/PS1 mice and APP-SH-SY5Y cells. [Abstract]2019 Mar 15:221:35-46. PMID: 30735733 -
Life Metab
Intermittent fasting inhibits platelet activation and thrombosis through the intestinal metabolite indole-3-propionate. [Abstract]2025 Jan 29;4(2):loaf002. PMID: 40078933 -
Bioeng Transl Med
2023 Oct 7;9(1):e10603. PMID: 38193124 -
EMBO Rep
GAPDH facilitates homologous recombination repair by stabilizing RAD51 in an HDAC1-dependent manner. [Abstract]2023 Aug 3;24(8):e56437. PMID: 37306047 -
Cells
Nanospheres Loaded with Curcumin Improve the Bioactivity of Umbilical Cord Blood-Mesenchymal Stem Cells via c-Src Activation During the Skin Wound Healing Process. [Abstract]2020 Jun 15;9(6):1467. PMID: 32549381 -
Cells
Nanosphere Loaded with Curcumin Inhibits the Gastrointestinal Cell Death Signaling Pathway Induced by the Foodborne Pathogen Vibrio vulnificus. [Abstract]2020 Mar 5;9(3):631. PMID: 32151068 -
mBio
ATP1A1 enhances porcine reproductive and respiratory syndrome virus type 2 attachment and internalization. [Abstract]2026 Apr 8;17(4):e0389625. PMID: 41773865 -
Chem Biol Interact
Aristolochic acid I induced mitochondrial Ca2+ accumulation triggers the production of MitoROS and activates Src/FAK pathway in hepatocellular carcinoma cells. [Abstract]2025 Jan 5:405:111269. PMID: 39426658 -
mSystems
Increasing the Hindgut Carbohydrate/Protein Ratio by Cecal Infusion of Corn Starch or Casein Hydrolysate Drives Gut Microbiota-Related Bile Acid Metabolism To Stimulate Colonic Barrier Function. [Abstract]2020 Jun 2;5(3):e00176-20. PMID: 32487741 -
PLoS Pathog
The protein segregase VCP/p97 promotes host antifungal defense via regulation of SYK activation. [Abstract]2024 Oct 29;20(10):e1012674. PMID: 39471181 -
Cancer Sci
c-Src inhibitor selectively inhibits triple-negative breast cancer overexpressed Vimentin in vitro and in vivo. [Abstract]2018 May;109(5):1648-1659. PMID: 29575318
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.
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J Cell Mol Med
ZEB1-mediated vasculogenic mimicry formation associates with epithelial-mesenchymal transition and cancer stem cell phenotypes in prostate cancer. [Abstract]2018 Aug;22(8):3768-3781. PMID: 29754422
PP2 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Aug;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.
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FASEB J
Src-mediated phosphorylation of GAPDH regulates its nuclear localization and cellular response to DNA damage. [Abstract]2020 Aug;34(8):10443-10461. PMID: 32539222
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.
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J Virol
Pseudorabies Virus Regulates the Extracellular Translocation of Annexin A2 To Promote Its Proliferation. [Abstract]2023 Mar 30;97(3):e0154522. PMID: 36786600 -
Nanotoxicology
Polystyrene nanoplastics promote tumor lung metastasis by inducing sodium overload in macrophages in an NMDAR-dependent way. [Abstract]2026 May 19:1-18. PMID: 42154607 -
Reprod Toxicol
Protective effect of ginsenoside Rg3 on DBP-induced spermatogenesis injury via the Src/PI3K signaling pathway. [Abstract]2025 Sep 8:109047. PMID: 40930195 -
FEBS Lett
2020 Jul;594(14):2294-2302. PMID: 32412649 -
Steroids
Cardiac steroid ouabain transcriptionally increases human leukocyte antigen DR expression on monocytes. [Abstract]2021 Nov:175:108915. PMID: 34508735 -
Eur J Neurosci
Phosphorylation of NMDA receptor GluN2B subunit at Tyr1472 is important for trigeminal processing of itch. [Abstract]2016 Oct;44(7):2474-2482. PMID: 27422716 -
J Biochem
Upregulated mGluR5 induces ER stress and DNA damage by regulating the NMDA receptor subunit NR2B. [Abstract]2022 Mar 3;171(3):349-359. PMID: 34908130 -
Neurol Res
Exploring neuroprotective effects of PP2 in ischemic stroke via bioinformatics and experimental validation. [Abstract]2025 Sep;47(9):864-875. PMID: 40355807 -
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bioRxiv
A Hotspot Phosphorylation Site on SHP2 Drives Oncoprotein Activation and Drug Resistance. [Abstract]2025 Jun 16:2025.06.11.659120. PMID: 40667115 -
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Bioengineered
Proto-oncogene tyrosine-protein kinase SRC (Src) inhibition in microglia relieves neuroinflammation in neuropathic pain mouse models. [Abstract]2021 Dec;12(2):11390-11398. PMID: 34851237 -
Oncotarget
2017 Nov 22;8(65):109135-109150. PMID: 29312596
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.
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Zhonghua Wei Zhong Bing Ji Jiu Yi Xue
[Research on the effect of protection against ventilator-induced lung injury via regulation of caveolin-1/heme oxygenase-1 signaling]. [Abstract]2015 Jul;27(7):568-73. PMID: 26138418
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
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[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]
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 | Concentration Solvent Mass | 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 |