Name: SCH772984
Price: 407.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    SCH772984, identified by an affinity-based mass spectroscopy high-throughput platform, is a novel, potent and ATP-competitive inhibition of ERK1 and ERK2 with 50% inhibition concentration IC50 values of 4 nmol/L and 1 nmol/L respectively. Although it displays behaviors of both type I and type II kinase inhibitors, SCH772984 is highly selective against only seven kinases, including CLK2, FLT4, GSG2, MAP4K4, MAPK1, MINK1, PRKD1 and TTK, out of a wide range of 300 tested with more than 50% inhibition at a concentration of 1 μmol/L. Study results have shown that SCH772984 potently inhibits tumor cells with mutations in BRAF, NRAS and KRAS at nanomolar concentrations.
- Properties
  - Alternative Name
    
    SCH 772984; SCH-772984; (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
    
    CAS Number
    
    942183-80-4
    
    Molecular Formula
    
    C33H33N9O2
    
    Molecular Weight
    
    587.67
    
    Appearance
    
    A solid
    
    Purity
    
    98.11%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥14.7 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. 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
    2. 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
    3. 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
    4. 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
    5. 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
    6. 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
    7. Linnan Yang, Jing Sun, et al. "Synergetic Functional Nanocomposites Enhance Immunotherapy in Solid Tumors by Remodeling the Immunoenvironment." Advanced Science. 16 February 2019.
    8. 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
    9. 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
    10. 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
    11. 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
    12. 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
    13. Ying-Ying Li. "BRAF inhibitor (vemurafenib) resistance confers sensitivity to arginine deprivation in melanoma." University of Miami.May 2016.

SCH772984

SCH772984

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