SCH772984

TargetMol
Product Code: TAR-T6066
Supplier: TargetMol
CodeSizePrice
TAR-T6066-2mg2mg£131.00
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TAR-T6066-5mg5mg£151.00
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TAR-T6066-1mL1 mL * 10 mM (in DMSO)£177.00
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TAR-T6066-10mg10mg£192.00
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TAR-T6066-25mg25mg£317.00
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TAR-T6066-50mg50mg£440.00
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Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

1 / 1

Further Information

Bioactivity:
SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases.
CAS:
942183-80-4
Formula:
C33H33N9O2
Molecular Weight:
587.67
Pathway:
MAPK
Purity:
0.9875
SMILES:
O=C(CN1CC[C@H](C1)C(=O)Nc1ccc2[nH]nc(-c3ccncc3)c2c1)N1CCN(CC1)c1ccc(cc1)-c1ncccn1
Target:
ERK; MEK

References

Zhu F D, Wang B D, Qin D L, et al.Carpesii fructus extract exhibits neuroprotective effects in cellular and Caenorhabditis elegans models of Parkinson's disease.CNS Neuroscience & Therapeutics.2023 Bin Y F, Ma N, Lu Y X, et al. Erythromycin reverses cigarette smoke extract-induced corticosteroid insensitivity by inhibition of the JNK/c-Jun pathway. Free Radical Biology and Medicine. 2020, 152: 494-503 Xie D, Ge X, Ma Y, et al. Clemastine improves hypomyelination in rats with hypoxic?ischemic brain injury by reducing microglia-derived IL-1? via P38 signaling pathway. Journal of neuroinflammation. 2020, 17(1): 1-17. Chang G, Xiao W, Xu Z, et al. Pterostilbene Induces Cell Apoptosis and Cell Cycle Arrest in T-Cell Leukemia/Lymphoma by Suppressing the ERK1/2 Pathway. BioMed Research International. 2017;2017:9872073 Caiola E, Iezzi A, Tomanelli M, et al. LKB1 deficiency renders non-small-cell lung cancer cells sensitive to ERK inhibitors.: ERK inhibitors in LKB1 mutated NSCLC. Journal of Thoracic Oncology. 2019 Li M, Wang Z, Fu S, et al.Taurine reduction of injury from neutrophil infiltration ameliorates Streptococcus uberis-induced mastitis.International Immunopharmacology.2023, 124: 111028. Caiola E, Iezzi A, Tomanelli M, et al. LKB1 deficiency renders non-small-cell lung cancer cells sensitive to ERK inhibitors.: ERK inhibitors in LKB1 mutated NSCLC[J]. Journal of Thoracic Oncology. 2019. Wang X, Xie Q, Ji Y, et al.Targeting KRAS-mutant stomach/colorectal tumors by disrupting the ERK2-p53 complex.Cell Reports.2023, 42(1): 111972. Zhao Z, Xue F, Gu Y, et al. Crosstalk between the muscular estrogen receptor ? and BDNF/TrkB signaling alleviates metabolic syndrome via 7, 8-dihydroxyflavone in female mice. Molecular Metabolism. 2020: 101149. Zhao Z, Xue F, Gu Y, et al. Crosstalk between the muscular estrogen receptor ? and BDNF/TrkB signaling alleviates metabolic syndrome via 7, 8-dihydroxyflavone in female mice[J]. Molecular Metabolism. 2020: 101149. Bin Y F, Ma N, Lu Y X, et al. Erythromycin reverses cigarette smoke extract-induced corticosteroid insensitivity by inhibition of the JNK/c-Jun pathway[J]. Free Radical Biology and Medicine. 2020, 152: 494-503. Lai J, Li Y, Ran M, et al.Xanthotoxin, a novel inducer of platelet formation, promotes thrombocytopoiesis via IL-1R1 and MEK/ERK signaling.Biomedicine & Pharmacotherapy.2023, 163: 114811. Zeng F, Li Y, Deng Z, et al. SARS?CoV?2 Spike Spurs Intestinal Inflammation via VEGF Production in Enterocytes. EMBO Molecular Medicine. 2022 May 9;14(5):e14844. doi: 10.15252/emmm.202114844. Epub 2022 Apr 19. Jiang S, Wang Z, Zhu T, et al. The Downregulation of EIF3a Contributes to Vemurafenib Resistance in Melanoma By Activating ERK Via PPP2R1B. Frontiers in Pharmacology. 2021: 2242. Zhang B, Zhao J, Wang Z, et al. DL0410 attenuates oxidative stress and neuroinflammation via BDNF/TrkB/ERK/CREB and Nrf2/HO-1 activation[J]. International Immunopharmacology. 2020, 86: 106729. Xie D, Ge X, Ma Y, et al. Clemastine improves hypomyelination in rats with hypoxic?ischemic brain injury by reducing microglia-derived IL-1? via P38 signaling pathway[J]. Journal of neuroinflammation. 2020, 17(1): 1-17. Lang J Y, Wang X, Xie Q, et al. Targeting KRAS-mutant stomach/colorectal tumours by disrupting the ERK2-p53 complex[J]. bioRxiv. 2020 Jiang S, Wang Z, Zhu T, et al. The Downregulation of EIF3a Contributes to Vemurafenib Resistance in Melanoma By Activating ERK Via PPP2R1B[J]. 2021 Zhang B, Zhao J, Wang Z, et al. DL0410 attenuates oxidative stress and neuroinflammation via BDNF/TrkB/ERK/CREB and Nrf2/HO-1 activation. International Immunopharmacology. 2020, 86: 106729. Chang G, Xiao W, Xu Z, et al. Pterostilbene Induces Cell Apoptosis and Cell Cycle Arrest in T-Cell Leukemia/Lymphoma by Suppressing the ERK1/2 Pathway[J]. BioMed Research International. 2017;2017:9872073 Yang J, Wang X, Fan Y, et al. Tropoelastin improves adhesion and migration of intra-articular injected infrapatellar fat pad MSCs and reduces osteoarthritis progression. Bioactive Materials. 2021 Chaikuad A, et al. A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nat Chem Biol. 2014 Oct;10(10):853-60. Caiola E, Iezzi A, Tomanelli M, et al. LKB1 Deficiency Renders NSCLC Cells Sensitive to ERK Inhibitors. Journal of Thoracic Oncology. 2020, 15(3): 360-370 Morris EJ, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-50. Chang Y W, Wang C C, Yin C F, et al. Quantitative phosphoproteomics reveals ectopic ATP synthase on mesenchymal stem cells to promote tumor progression via ERK/c-Fos pathway activation. Molecular & Cellular Proteomics. 2022, 21(6)