PP 2 (AG 1879)
(Synonyms: AGL 1879) 目录号 : GC10344
PP 2 (AG 1879)是一种选择性Src家族激酶抑制剂。PP 2抑制Lck和Fyn的半数抑制浓度（IC50）分别为0.004μM和0.005μM。
Cas No.:172889-27-9
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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.
PP 2 (AG 1879)是一种选择性Src家族激酶抑制剂[1]。PP 2抑制Lck和Fyn的半数抑制浓度（IC50）分别为0.004μM和0.005μM[2]。
在体外实验中，PP 2（10μM; 30分钟）可抑制PrP106-126诱导的、通过CD36介导的BV2小胶质细胞中iNOS的激活[3]。PP 2（5, 10或20μM; 24, 48或72小时）可抑制头颈部鳞状细胞癌（HNSCC）细胞系的生长，并诱导其凋亡[4]。
在体内实验中，PP 2（2mg/kg; 8周; 腹腔注射）通过调节NF-κB/COX-2和PPARγ/UCP2通路，在糖尿病小鼠中可改善肾纤维化[1]。PP 2（1mg/kg; 4天; 腹腔注射）通过抑制Src激酶，在雄性小鼠中可保护机体免受角蛋白突变相关的肝脏损伤和丝状结构破坏[5]。
| 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 | |
| 别名 | AGL 1879 | ||
| 化学名 | 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 | ||
| 分子式 | C15H16ClN5 | 分子量 | 301.78 |
| 溶解度 | ≥ 15.1mg/mL in DMSO, ≥ 20.05 mg/mL in EtOH with ultrasonic | 储存条件 | Desiccate at 4°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet