SCH772984 (CAS 942183-80-4)
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SCH772984 is an innovative inhibitor that selectively targets kinases 1 and 2 (ERK1/2), exhibiting characteristics of both type I and type II kinase inhibitors. ERK1/2 are redundant kinases activated by various growth factors and mitogens. This compound demonstrates high selectivity, with only seven kinases out of 300 tested exhibiting more than 50% inhibition at a concentration of 1 µM. SCH772984 shows potent cytotoxicity in tumor cells carrying BRAF, NRAS, or KRAS mutations, with nanomolar efficacy. One of the distinctive features of SCH772984 is its slow binding kinetics, as it binds to an inactive ERK isoform in a novel binding pocket. This compound has shown promising anticancer properties against melanoma, particularly in BRAF mutant, NRAS mutant, and wild-type cell cultures. Combining SCH772984 with vemurafenib in BRAF mutant melanoma has demonstrated synergistic effects across the majority of cell lines, effectively delaying the onset of acquired resistance in long-term in vitro assays.
SCH772984 (CAS 942183-80-4) References
- Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. | Morris, EJ., et al. 2013. Cancer Discov. 3: 742-50. PMID: 23614898
- Antitumor activity of the ERK inhibitor SCH772984 [corrected] against BRAF mutant, NRAS mutant and wild-type melanoma. | Wong, DJ., et al. 2014. Mol Cancer. 13: 194. PMID: 25142146
- Dissecting Therapeutic Resistance to ERK Inhibition. | Jha, S., et al. 2016. Mol Cancer Ther. 15: 548-59. PMID: 26832798
- Analgesic effect and possible mechanism of SCH772984 intrathecal injection on rats with bone cancer pain. | Bian, J., et al. 2016. Saudi Pharm J. 24: 354-62. PMID: 27275127
- Phenformin Enhances the Efficacy of ERK Inhibition in NF1-Mutant Melanoma. | Trousil, S., et al. 2017. J Invest Dermatol. 137: 1135-1143. PMID: 28143781
- Human primary liver cancer-derived organoid cultures for disease modeling and drug screening. | Broutier, L., et al. 2017. Nat Med. 23: 1424-1435. PMID: 29131160
- Cucurbitacin B and SCH772984 exhibit synergistic anti-pancreatic cancer activities by suppressing EGFR, PI3K/Akt/mTOR, STAT3 and ERK signaling. | Zhou, J., et al. 2017. Oncotarget. 8: 103167-103181. PMID: 29262554
- DL0410 attenuates oxidative stress and neuroinflammation via BDNF/TrkB/ERK/CREB and Nrf2/HO-1 activation. | Zhang, B., et al. 2020. Int Immunopharmacol. 86: 106729. PMID: 32645628
- GIT1 overexpression promotes epithelial-mesenchymal transition and predicts poor prognosis in hepatocellular carcinoma. | Wang, G., et al. 2021. Bioengineered. 12: 30-43. PMID: 33258389
- Extracellular signal-regulated kinase inhibition prevents venous adaptive remodeling via regulation of Eph-B4. | Guo, Y., et al. 2022. Vascular. 30: 120-129. PMID: 33706642
- Selective Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibition by the SCH772984 Compound Attenuates In Vitro and In Vivo Inflammatory Responses and Prolongs Survival in Murine Sepsis Models. | Kopczynski, M., et al. 2021. Int J Mol Sci. 22: PMID: 34638546
- LAGE3 promoted cell proliferation, migration, and invasion and inhibited cell apoptosis of hepatocellular carcinoma by facilitating the JNK and ERK signaling pathway. | Xing, Y., et al. 2021. Cell Mol Biol Lett. 26: 49. PMID: 34837962
- Indazole Derivatives Effective against Gastrointestinal Diseases. | Saha, S., et al. 2022. Curr Top Med Chem. 22: 1189-1214. PMID: 34886775
- FOXD1-dependent RalA-ANXA2-Src complex promotes CTC formation in breast cancer. | Long, Y., et al. 2022. J Exp Clin Cancer Res. 41: 301. PMID: 36229838
- The role of P21-activated kinase (Pak1) in sinus node function. | Pereira, CH., et al. 2023. J Mol Cell Cardiol.. PMID: 37086972
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SCH772984, 5 mg | sc-473205 | 5 mg | $363.00 |