![](/_next/image?url=https%3A%2F%2Fresource.apexbio.cn%2Fapexbio%2Fproduct%2FA3805%2Fa3805.png&w=3840&q=75)
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥2000.00 | 现货 | |
5mg | ¥1090.00 | 现货 | |
10mg | ¥1636.00 | 现货 | |
25mg | ¥3272.00 | 现货 | |
50mg | ¥5818.00 | 现货 |
特色产品
![Cy5 TSA Fluorescence System Kit](/_next/image?url=https%3A%2F%2Fresource.apexbio.cn%2Fapexbio%2Fbanner%2FK1038%EF%BC%8CK1050-K1052_1.png&w=3840&q=75)
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
![EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)](/_next/image?url=https%3A%2F%2Fresource.apexbio.cn%2Fapexbio%2Fbanner%2FK1079-K1081_1.png&w=3840&q=75)
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
SCH772984,通过基于亲和力的质谱高通量平台而鉴定到,是一种新型有效的和ATP竞争性的ERK1和ERK2抑制剂,IC50值分别为4 nmol/L和1 nmol/L。尽管SCH772984具有I型和II型激酶抑制剂的行为,但在300个激酶的实验中,SCH772984只对7种激酶具有高选择性,包括CLK2、FLT4、GSG2、MAP4K4、MAPK1、MINK1、PRKD1和TTK,在1 μmol/L浓度时具有超过50%的抑制。研究结果表明,SCH772984在纳摩尔浓度时有效抑制含BRAF、NRAS和KRAS突变的肿瘤细胞的生长。
参考文献:
Morris EJ, Jha S, Restaino CR, Dayananth P, Zhu H, Cooper A, Carr D, Deng Y, Jin W, Black S, Long B, Liu J, Dinunzio E, Windsor W, Zhang R, Zhao S, Angagaw MH, Pinheiro EM, Desai J, Xiao L, Shipps G, Hruza A, Wang J, Kelly J, Paliwal S, Gao X, Babu BS, Zhu L, Daublain P, Zhang L, Lutterbach BA, Pelletier MR, Philippar U, Siliphaivanh P, Witter D, Kirschmeier P, Bishop WR, Hicklin D, Gilliland DG, Jayaraman L, Zawel L, Fawell S, Samatar AA. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-750
产品性质
物理外观 | A solid |
CAS号 | 942183-80-4 |
分子式 | C33H33N9O2 |
分子量 | 587.67 |
化学名称 | (3R)-1-[2-oxo-2-[4-(4-pyrimidin-2-ylphenyl)piperazin-1-yl]ethyl]-N-(3-pyridin-4-yl-1H-indazol-5-yl)pyrrolidine-3-carboxamide |
溶解度 | insoluble in EtOH; insoluble in H2O; ≥14.7 mg/mL in DMSO with gentle warming |
SMILES | C1CN(CC1C(=O)NC2=CC3=C(C=C2)NN=C3C4=CC=NC=C4)CC(=O)N5CCN(CC5)C6=CC=C(C=C6)C7=NC=CC=N7 |
存储条件 | -20°C |
运输条件 | 蓝冰 |
SDF文件 | Download SDF |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
生物活性描述 | SCH772984是一种新型特异性的ERK1/2抑制剂,IC50值分别为4 nM和1 nM。 | |
靶点 | ERK1 | ERK2 |
生物活性数据 | 4 nM | 1 nM |
生物相关数据
质量控制
操作说明
产品引用文献
- 1. Guoyue Lv, et al. "Activation of GPR3-β-arrestin2-PKM2 pathway in Kupffer cells stimulates glycolysis and inhibits obesity and liver pathogenesis." Nat Commun. 2024 Jan 27;15(1):807. PMID: 38280848
- 2. Jinchao Gao, Qingxiang Song, et al. "Intracerebral fate of organic and inorganic nanoparticles is dependent on microglial extracellular vesicle function." Nat Nanotechnol. 2024 Mar;19(3):376-386. PMID: 38158436
- 3. Shengliang Zhang, Lanlan Zhou, et al. "Small-molecule NSC59984 induces mutant p53 degradation through a ROS-ERK2-MDM2 axis in cancer cells." Mol Cancer Res. 2022 Jan 6. PMID: 34992144
- 4. Xin‐Li Liu, Wen‐Jing Liu, et al. "miR-506-loaded gelatin nanospheres target PENK and inactivate the ERK/Fos signaling pathway to suppress triple-negative breast cancer aggressiveness." Mol Carcinog. 2021 Aug;60(8):538-555. PMID: 34062009
- 5. Labuzan SA, Lynch SA, et al. "Inhibition of Protein Phosphatase Methylesterase 1 Dysregulates MAP Kinase Signaling and Attenuates Muscle Cell Differentiation." Gene. 2020;144515. PMID: 32112987
- 6. Liu B, Shen LJ, et al. "Automobile exhaust-derived PM(2.5) induces blood-testis barrier damage through ROS-MAPK-Nrf2 pathway in sertoli cells of rats." Ecotoxicol Environ Saf. 2020 Feb;189:110053. PMID: 31862514
- 7. Li J, Shi W, et al. "Activation of DR3 signaling causes loss of ILC3s and exacerbates intestinal inflammation." Nat Commun. 2019 Jul 29;10(1):3371. PMID: 31358760
- 8. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID: 31063758
- 9. Linnan Yang, Jing Sun, et al. "Synergetic Functional Nanocomposites Enhance Immunotherapy in Solid Tumors by Remodeling the Immunoenvironment." Advanced Science. 16 February 2019.
- 10. Wang Q, Zhi Y, et al. "Suppression of OSCC malignancy by oral glands derived-PIP identified by iTRAQ combined with 2D LC-MS/MS." J Cell Physiol. 2019 Jan 28. PMID: 30693510
- 11. Alhakeem SS, McKenna MK, et al. "Chronic Lymphocytic Leukemia-Derived IL-10 Suppresses Antitumor Immunity." J Immunol. 2018 Jun 15;200(12):4180-4189. PMID: 29712773
- 12. Li YY, Wu C, et al. "Degradation of AMPK-α1 sensitizes BRAF inhibitor-resistant melanoma cells to arginine deprivation." Mol Oncol. 2017 Dec;11(12):1806-1825. PMID: 29094484
- 13. Stark RJ, Koch SR, et al."Endothelial nitric oxide synthase modulates Toll-like receptor 4-mediated IL-6 production and permeability via nitric oxide-independent signaling." FASEB J. 2017 Oct 23. pii: fj.201700410R. PMID: 29061842
- 14. Ferraiuolo RM, Tubman J, et al. "The cyclin-like protein, SPY1, regulates the ERα and ERK1/2 pathways promoting tamoxifen resistance."Oncotarget. 2017 Apr 4;8(14):23337-23352. PMID: 28423577
- 15. Ying-Ying Li. "BRAF inhibitor (vemurafenib) resistance confers sensitivity to arginine deprivation in melanoma." University of Miami. May 2016.