PP 2 (AG 1879) (Synonyms: AGL 1879) |
| رقم الكتالوجGC10344 |
PP 2 (AG 1879) is a selective Src family kinase inhibitor. The IC50 values of PP 2 for inhibiting Lck and Fyn are 0.004μM and 0.005μM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 172889-27-9
Sample solution is provided at 25 µL, 10mM.
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PP 2 (AG 1879) is a selective Src family kinase inhibitor[1]. The IC50 values of PP 2 for inhibiting Lck and Fyn are 0.004μM and 0.005μM, respectively[2].
In vitro, PP 2 (10μM; 30min) inhibits PrP106-126-induced iNOS activation mediated by CD36 in BV2 microglia[3]. PP 2 (5, 10 or 20μM; 24, 48 or 72 h) suppresses growth and induces apoptosis in HNSCC cell lines[4].
In vivo, PP 2 (2mg/kg; 8 weeks; i.p.) ameliorates renal fibrosis by regulating the NF-κB/COX-2 and PPAR γ/UCP2 pathway in diabetic mice[1]. PP 2 (1mg/kg; 4 days; i.p.) protects from keratin mutation–associated liver injury and filament disruption via SRC kinase inhibition in male mice[5].
References:
[1] Wei J, Deng X, Li Y, et al. PP2 Ameliorates Renal Fibrosis by Regulating the NF-κB/COX-2 and PPARγ/UCP2 Pathway in Diabetic Mice. Oxid Med Cell Longev. 2021 Sep 17;2021:7394344.
[2] Hanke JH, Gardner JP, Dow RL, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701.
[3] Zhang S, Yang L, Kouadir M, et al. PP2 and piceatannol inhibit PrP106-126-induced iNOS activation mediated by CD36 in BV2 microglia. Acta Biochim Biophys Sin (Shanghai). 2013 Sep;45(9):763-72.
[4] Lee S, Park S, Ryu JS, et al. c-Src inhibitor PP2 inhibits head and neck cancer progression through regulation of the epithelial-mesenchymal transition. Exp Biol Med (Maywood). 2023 Mar;248(6):492-500.
[5] Li P, Maitra D, Kuo N, et al. PP2 protects from keratin mutation-associated liver injury and filament disruption via SRC kinase inhibition in male but not female mice. Hepatology. 2023 Jan 1;77(1):144-158.
| Cell experiment [1]: | |
Cell lines | YD9, YD15, YD10-B, SNU1076, SNU46, SNU899, and SNU1041 |
Preparation Method | Cells were seeded into 96-well plates at a density of 5 × 103 cells/well and allowed to reach confluence. Cells were then exposed to PP 2 at the indicated concentrations (5, 10 or 20μM) for 24, 48 or 72 h. After exposure, cell viability was assessed using a cell counting kit-8 following the protocol provided with the kit. Briefly, CCK8 solution was added to the wells containing the cell suspension, and the plates were incubated for 1h. Subsequently, the optical density was measured using the Bio-Tek microplate reader. Data are presented as a percentage relative to the control cells. |
Reaction Conditions | 5, 10 or 20μM; 24, 48 or 72 h |
Applications | PP 2 suppresses growth and induces apoptosis in HNSCC cell lines. |
| Animal experiment [2]: | |
Animal models | Four-to six-week-old F22 male and female mice |
Preparation Method | Four-to six-week-old F22 male and female mice on an FVB/N background expressing the human K18 R90C mutant were used. Mice received daily intraperitoneal injections of PP 2 (1mg/kg) or DMSO for 4 days. For immunofluorescence experiments, livers were collected after CO2 euthanasia, embedded in optimal cutting temperature compound, and stored at -80°C. For Fas experiments, mice were treated with an intraperitoneal injection of Fas antibody (0.15μg/g). After 5h, mice were sacrificed, and blood and livers were collected. Livers were fixed in 10% formalin and analyzed by hematoxylin and eosin (H&E) staining or terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) assay. Hemorrhage scores were calculated using QuPath (Quantitative Pathology & Bioimage Analysis) and ImageJ software. Apoptosis was estimated using the TUNEL assay detection kit (ApopTag Peroxidase In Situ Apoptosis). Fluorescence images were acquired with the same exposure time and used to count apoptotic nuclei. Serum alanine aminotransferase (ALT) levels were determined using the Liquid ALT Reagent Set. For acetaminophen (APAP) experiments, a 0-4 scoring system was used to determine the liver histopathology score. |
Dosage form | 1mg/kg; 4 days; i.p. |
Applications | PP 2 protects from keratin mutation–associated liver injury and filament disruption via SRC kinase inhibition in male mice. |
References: | |
| Cas No. | 172889-27-9 | SDF | |
| المرادفات | AGL 1879 | ||
| Chemical Name | 1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine | ||
| Canonical SMILES | CC(C)(C)N1C2=C(C(=N1)C3=CC=C(C=C3)Cl)C(=NC=N2)N | ||
| Formula | C15H16ClN5 | M.Wt | 301.78 |
| الذوبان | ≥ 15.1mg/mL in DMSO, ≥ 20.05 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3137 mL | 16.5684 mL | 33.1367 mL |
| 5 mM | 662.7 μL | 3.3137 mL | 6.6273 mL |
| 10 mM | 331.4 μL | 1.6568 mL | 3.3137 mL |
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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 ddH2O, 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%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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