Molecular structure of GSK-3β Inhibitor VIII, CAS Number: 487021-52-3
GSK-3β Inhibitor VIII (CAS 487021-52-3)
See product citations (5)
Alternate Names:
AR-A014418; N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea
Application:
GSK-3β Inhibitor VIII is a potent, selective inhibitor of GSK-3β
CAS Number:
487021-52-3
Purity:
>95%
Molecular Weight:
308.3
Molecular Formula:
C12H12N4O4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GSK-3β Inhibitor VIII is a cell-permeable, potent, and selective inhibitor of GSK-3beta. Inhibition is competitive with respect to ATP, and unlike other GSK3 inhibitors, this compound does not inhibit of cyclin dependent kinases. GSK-3β Inhibitor VIII has also been shown to inhibit translocation of the NFAT (nuclear factor of activated T-cells) family of transcription factors, expressed in most immune system cells, which are regulators of cellular differentiation and proliferation. GSK-3β Inhibitor VIII has also been shown to protect neuronal cells against Ab-mediated neurodegeneration in vitro and reduce tauopathy.
GSK-3β Inhibitor VIII (CAS 487021-52-3) References
- NFAT signaling: choreographing the social lives of cells. | Crabtree, GR. and Olson, EN. 2002. Cell. 109 Suppl: S67-79. PMID: 11983154
- Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. | Bhat, R., et al. 2003. J Biol Chem. 278: 45937-45. PMID: 12928438
- AR-A014418, a selective GSK-3 inhibitor, produces antidepressant-like effects in the forced swim test. | Gould, TD., et al. 2004. Int J Neuropsychopharmacol. 7: 387-90. PMID: 15315719
- Inhibition of glycogen synthase kinase-3 by lithium correlates with reduced tauopathy and degeneration in vivo. | Noble, W., et al. 2005. Proc Natl Acad Sci U S A. 102: 6990-5. PMID: 15867159
- Synthesis and ex vivo evaluation of carbon-11 labelled N-(4-methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl)urea ([11C]AR-A014418): a radiolabelled glycogen synthase kinase-3beta specific inhibitor for PET studies. | Vasdev, N., et al. 2005. Bioorg Med Chem Lett. 15: 5270-3. PMID: 16202587
- The antinociceptive effects of AR-A014418, a selective inhibitor of glycogen synthase kinase-3 beta, in mice. | Martins, DF., et al. 2011. J Pain. 12: 315-22. PMID: 20705523
- Towards the preparation of radiolabeled 1-aryl-3-benzyl ureas: Radiosynthesis of [(11)C-carbonyl] AR-A014418 by [(11)C]CO(2) fixation. | Hicks, JW., et al. 2012. Bioorg Med Chem Lett. 22: 2099-101. PMID: 22321216
- Glycogen synthase kinase 3-specific inhibitor AR-A014418 decreases neuropathic pain in mice: evidence for the mechanisms of action. | Mazzardo-Martins, L., et al. 2012. Neuroscience. 226: 411-20. PMID: 23000630
- AR-A014418 as a glycogen synthase kinase-3 inhibitor: anti-apoptotic and therapeutic potential in experimental spinal cord injury. | Tunçdemir, M., et al. 2013. Neurocirugia (Astur). 24: 22-32. PMID: 23116585
- Glycogen synthase kinase-3 inhibitor AR-A014418 suppresses pancreatic cancer cell growth via inhibition of GSK-3-mediated Notch1 expression. | Kunnimalaiyaan, S., et al. 2015. HPB (Oxford). 17: 770-6. PMID: 26147011
- GSK3 inhibitor AR-A014418 promotes osteogenic differentiation of human adipose-derived stem cells via ERK and mTORC2/Akt signaling pathway. | Zhang, M., et al. 2017. Biochem Biophys Res Commun. 490: 182-188. PMID: 28602697
- GSK3β suppression inhibits MCL1 protein synthesis in human acute myeloid leukemia cells. | Lee, YC., et al. 2021. J Cell Physiol. 236: 570-586. PMID: 32572959
- Personalized drug testing in human pheochromocytoma/paraganglioma primary cultures. | Wang, K., et al. 2022. Endocr Relat Cancer. 29: 285-306. PMID: 35324454
- AR-A014418 regulates intronic polyadenylation and transcription of PD-L1 through inhibiting CDK12 and CDK13 in tumor cells. | Zhang, G., et al. 2023. J Immunother Cancer. 11: PMID: 37164450
- Mitogen inactivation of glycogen synthase kinase-3 beta in intact cells via serine 9 phosphorylation. | Stambolic, V. and Woodgett, JR. 1994. Biochem J. 303 (Pt 3): 701-4. PMID: 7980435
Inhibitor of:
BC061212, Enzyme, FAM48B2, GCK, GCP5, GSK-3 beta, GSKIP, nArgBP2, X11γ, and YSK1.Activator of:
4931431F19Rik, casein kinase Iγ1, Collapsin response mediator protein (CRMP), Neurotrypsin, Prickle4, TNIK, and TTBK2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK-3β Inhibitor VIII, 5 mg | sc-202636 | 5 mg | $134.00 | |||
GSK-3β Inhibitor VIII, 10 mg | sc-202636A | 10 mg | $150.00 |