GSK360A (CAS 931399-19-8)
See product citations (1)
QUICK LINKS
GSK360A is a selective and potent inhibitor of ETV6-NTRK3 (EN), a fusion protein that plays a critical role in the signaling pathways involved in cellular proliferation and differentiation. This compound operates by specifically targeting and binding to the ATP-binding site of the EN fusion kinase, effectively blocking its kinase activity. By inhibiting this kinase activity, GSK360A disrupts the downstream signaling pathways that are essential for the tumorigenic and proliferative processes in cells expressing the ETV6-NTRK3 fusion protein. Its mechanism of action provides useful for researchers studying the role of EN in various cellular processes, including cell cycle regulation, apoptosis, and cell differentiation. In scientific studies, GSK360A has been utilized to understand the biological consequences of EN inhibition in cellular models, offering insights into the potential pathways through which EN contributes to cellular transformation and proliferation. Its use in research applications facilitates the exploration of novel therapeutic targets and the elucidation of complex signaling networks that underlie various forms of cancer.
GSK360A (CAS 931399-19-8) References
- Chronic inhibition of hypoxia-inducible factor prolyl 4-hydroxylase improves ventricular performance, remodeling, and vascularity after myocardial infarction in the rat. | Bao, W., et al. 2010. J Cardiovasc Pharmacol. 56: 147-55. PMID: 20714241
- Unfavourable consequences of chronic cardiac HIF-1α stabilization. | Hölscher, M., et al. 2012. Cardiovasc Res. 94: 77-86. PMID: 22258630
- Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis. | Beuck, S., et al. 2012. Drug Test Anal. 4: 830-45. PMID: 22362605
- HIF-prolyl hydroxylases and cardiovascular diseases. | Sen Banerjee, S., et al. 2012. Toxicol Mech Methods. 22: 347-58. PMID: 22424133
- Hypoxia-inducible factor as a therapeutic target for cardioprotection. | Ong, SG. and Hausenloy, DJ. 2012. Pharmacol Ther. 136: 69-81. PMID: 22800800
- Molecular mechanisms of action and therapeutic uses of pharmacological inhibitors of HIF-prolyl 4-hydroxylases for treatment of ischemic diseases. | Selvaraju, V., et al. 2014. Antioxid Redox Signal. 20: 2631-65. PMID: 23992027
- HIF-1 reduces ischaemia-reperfusion injury in the heart by targeting the mitochondrial permeability transition pore. | Ong, SG., et al. 2014. Cardiovasc Res. 104: 24-36. PMID: 25063991
- Pharmacological targeting of the HIF hydroxylases--A new field in medicine development. | Chan, MC., et al. 2016. Mol Aspects Med. 47-48: 54-75. PMID: 26791432
- Hypoxia-inducible factor prolyl 4-hydroxylase inhibition in cardiometabolic diseases. | Koivunen, P., et al. 2016. Pharmacol Res. 114: 265-273. PMID: 27832958
- The prolyl 4-hydroxylase inhibitor GSK360A decreases post-stroke brain injury and sensory, motor, and cognitive behavioral deficits. | Zhou, J., et al. 2017. PLoS One. 12: e0184049. PMID: 28880966
- Hypoxia-inducible factor 1 signalling, metabolism and its therapeutic potential in cardiovascular disease. | Sousa Fialho, MDL., et al. 2019. Biochim Biophys Acta Mol Basis Dis. 1865: 831-843. PMID: 30266651
- Hypoxia Inducible Factor-1α in Osteochondral Tissue Engineering. | Taheem, DK., et al. 2020. Tissue Eng Part B Rev. 26: 105-115. PMID: 31774026
- Physiopathology of the Permeability Transition Pore: Molecular Mechanisms in Human Pathology. | Bonora, M., et al. 2020. Biomolecules. 10: PMID: 32635556
- Brain-targeted hypoxia-inducible factor stabilization reduces neonatal hypoxic-ischemic brain injury. | Kuan, CY., et al. 2021. Neurobiol Dis. 148: 105200. PMID: 33248237
- A small-molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase improves obesity, nephropathy and cardiomyopathy in obese ZSF1 rats. | Signore, PE., et al. 2021. PLoS One. 16: e0255022. PMID: 34339435
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK360A, 5 mg | sc-490346 | 5 mg | $355.00 | |||
GSK360A, 10 mg | sc-490346A | 10 mg | $648.00 | |||
GSK360A, 25 mg | sc-490346B | 25 mg | $1474.00 | |||
GSK360A, 50 mg | sc-490346C | 50 mg | $2516.00 |