PP 1 (Synonyms: AGL 1872; EI 275) |
Catalog No.GC17990
One-Click Copy Product Info
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PP 1 is a novel, potent, and selective Src family tyrosine kinase inhibitor. PP 1 effectively inhibits the phosphorylation of Lck (IC50=5nM) and Fyn (IC50= 6nM) to block T-cell receptor signaling pathways.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 172889-26-8
Sample solution is provided at 25 µL, 10mM.
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PP 1 is a novel, potent, and selective Src family tyrosine kinase inhibitor. PP 1 effectively inhibits the phosphorylation of Lck (IC50=5nM) and Fyn (IC50= 6nM) to block T-cell receptor signaling pathways. PP 1 can be used in research related to cancers (such as small cell lung cancer and leukemia) as well as T-cell immune signal transduction[1-4].
In vitro, pretreatment of NMuMG/E9 mouse mammary epithelial cells with PP 1 (10μM) for 30min, followed by stimulation with TGF-β1 (1-5ng/mL) for 1-2 days. PP 1 significantly inhibited the occurrence of epithelial-mesenchymal transition (EMT), while preventing alterations in cell morphology, focal adhesion formation, and the activation of Smad2/3[5]. Pretreatment of human coronary artery smooth muscle cells (HCASMCs) and Swiss 3T3 cells with PP 1 (0.1–10μM) for 15min–4h, followed by stimulation with PDGF-BB (10–15ng/mL) for 4–20h. PP 1 significantly inhibited cell migration and proliferation, while reducing the tyrosine phosphorylation level of PDGFβ receptors[6].
In vivo, a single intraperitoneal injection of PP 1 (1.5mg/kg) was administered to treat the transient middle cerebral artery occlusion (tMCAO) mouse model. PP 1 significantly rescued the FUNDC1-mediated neuronal mitophagy dysfunction caused by I/R injury[7]. Daily intraperitoneal injection of PP 1 (2mg/kg) was administered to the unilateral ureteral obstruction (UUO)-induced renal fibrosis mouse model for 3-14 days. PP 1 significantly reduced the deposition of extracellular matrix and inhibited the activation of renal interstitial fibroblasts, thereby ameliorating the development of renal fibrosis[8].
References:
[1] Zan L, Zhang X, Xi Y, et al. Src regulates angiogenic factors and vascular permeability after focal cerebral ischemia-reperfusion. Neuroscience. 2014 Mar 14;262:118-28.
[2] Warmuth M, Simon N, Mitina O, et al. Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases. Blood. 2003 Jan 15;101(2):664-72.
[3] Karni R, Mizrachi S, Reiss-Sklan E, et al. The pp60c-Src inhibitor PP1 is non-competitive against ATP. FEBS Lett. 2003 Feb 27;537(1-3):47-52.
[4] Kantibekovna SL, Wang S, Kang H, et al. Selective antitumor and apoptosis‑inducing effects of the Src inhibitor PP1 in human tongue squamous cell carcinoma cells. Int J Oncol. 2026 May;68(5):64.
[5] Maeda M, Shintani Y, Wheelock MJ, et al. Src activation is not necessary for transforming growth factor (TGF)-beta-mediated epithelial to mesenchymal transitions (EMT) in mammary epithelial cells. PP1 directly inhibits TGF-beta receptors I and II. J Biol Chem. 2006 Jan 6;281(1):59-68.
[6] Waltenberger J, Uecker A, Kroll J, et al. A dual inhibitor of platelet-derived growth factor beta-receptor and Src kinase activity potently interferes with motogenic and mitogenic responses to PDGF in vascular smooth muscle cells. A novel candidate for prevention of vascular remodeling. Circ Res. 1999 Jul 9;85(1):12-22.
[7] Tang T, Hu LB, Ding C, et al. Src inhibition rescues FUNDC1-mediated neuronal mitophagy in ischaemic stroke. Stroke Vasc Neurol. 2024 Aug 27;9(4):367-379.
[8] Yan Y, Ma L, Zhou X, et al. Src inhibition blocks renal interstitial fibroblast activation and ameliorates renal fibrosis. Kidney Int. 2016 Jan;89(1):68-81.
| Cell experiment [1]: | |
Cell lines | NMuMG/E9 cells (mouse mammary epithelial cell line) |
Preparation Method | NMuMG/E9 cells were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 4.5g/L glucose, and 10μg/mL insulin. NMuMG/E9 cells were pretreated with PP 1 (10μM) for 30 minutes, followed by stimulation with TGF-β1 (1-5ng/mL) for up to 2 days. |
Reaction Conditions | 10μM; 30min pretreatment + TGF-β1 (1-5ng/mL) stimulation for up to 2 days |
Applications | PP 1 significantly prevented TGF-β1-mediated epithelial to mesenchymal transition (EMT) in NMuMG/E9 cells. PP 1 effectively inhibited TGF-β1-induced dissolution of cell-cell junctions and formation of stress fibers. Additionally, PP 1 suppressed the TGF-β1-induced expression of mesenchymal markers (such as N-cadherin and fibronectin) and the reduction of the epithelial marker ZO-1. PP 1 blocked the TGF-β1-induced transcriptional upregulation of N-cadherin, Snail, and SIP1, and inhibited the activation (tyrosine phosphorylation) of Src and its downstream substrates (including FAK, paxillin, and p120 catenin). |
| Animal experiment [2]: | |
Animal models | Mice (subjected to unilateral ureteral obstruction - UUO) |
Preparation Method | Mice were administered PP 1 (2mg/kg) via daily intraperitoneal injection for 7 or 14 days. Sham-operated and UUO vehicle-treated mice were used as controls. Mice were sacrificed at specified time points (days 3, 7, and 14) for tissue collection and analysis. |
Dosage form | 2mg/kg; i.p.; daily injection for 3-14 days |
Applications | PP 1 administration significantly reduced the deposition of extracellular matrix (ECM) proteins, as evidenced by Masson trichrome staining. PP 1 significantly inhibited the expression of fibronectin, collagen I, and α-smooth muscle actin (α-SMA), thereby attenuating UUO-induced renal fibrosis and activation of renal interstitial fibroblasts. PP 1 reduced the number of renal epithelial cells arrested at the G2/M phase of the cell cycle. |
References: | |
| Cas No. | 172889-26-8 | SDF | |
| Sinónimos | AGL 1872; EI 275 | ||
| Chemical Name | 1-tert-butyl-3-(4-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine | ||
| Canonical SMILES | CC1=CC=C(C=C1)C2=NN(C3=C2C(=NC=N3)N)C(C)(C)C | ||
| Formula | C16H19N5 | M.Wt | 281.36 |
| Solubility | ≥ 7.03mg/mL in DMSO, ≥ 20.6 mg/mL in EtOH with ultrasonic | Storage | Desiccate at 4°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5542 mL | 17.7708 mL | 35.5417 mL |
| 5 mM | 710.8 μL | 3.5542 mL | 7.1083 mL |
| 10 mM | 355.4 μL | 1.7771 mL | 3.5542 mL |
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)