GI 254023X (CAS 260264-93-5)
See product citations (1)
Alternate Names:
(2R)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-5-phenylpentanamide
Application:
GI 254023X is GI 254023X is an inhibitor of ADAM.
CAS Number:
260264-93-5
Molecular Weight:
391.5
Molecular Formula:
C21H33N3O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Product Citations
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
GI 254023X is a potent and selective inhibitor of the ADAM10 metalloprotease enzyme. It demonstrates significant activity against ADAM10 compared to ADAM17, with over 100-fold higher potency. In cell-based experiments, it effectively blocks the constitutive release of IL-6R, CX3CL1, and CXCL16, inhibits betacellulin shedding, prevents E-cadherin cleavage, and inhibits ADAM10-mediated neuronal outgrowth in vitro.
GI 254023X (CAS 260264-93-5) References
- Metalloproteinase inhibitors for the disintegrin-like metalloproteinases ADAM10 and ADAM17 that differentially block constitutive and phorbol ester-inducible shedding of cell surface molecules. | Ludwig, A., et al. 2005. Comb Chem High Throughput Screen. 8: 161-71. PMID: 15777180
- ADAM10 inhibition of human CD30 shedding increases specificity of targeted immunotherapy in vitro. | Eichenauer, DA., et al. 2007. Cancer Res. 67: 332-8. PMID: 17210715
- Improved synthesis of ADAM10 inhibitor GI254023X. | Hoettecke, N., et al. 2010. Neurodegener Dis. 7: 232-8. PMID: 20197648
- Soluble CD23 controls IgE synthesis and homeostasis in human B cells. | Cooper, AM., et al. 2012. J Immunol. 188: 3199-207. PMID: 22393152
- ADAM10 mediates N-cadherin ectodomain shedding during retinal ganglion cell differentiation in primary cultured retinal cells from the developing chick retina. | Paudel, S., et al. 2013. J Cell Biochem. 114: 942-54. PMID: 23129104
- Polycystin-1 and Gα12 regulate the cleavage of E-cadherin in kidney epithelial cells. | Xu, JX., et al. 2015. Physiol Genomics. 47: 24-32. PMID: 25492927
- [Effect of ADAM10 Inhibitor GI254023X on Proliferation and Apoptosis of Acute T-Lymphoblastic Leukemia Jurkat Cells In Vitro and Its Possible Mechanisms]. | Ma, S., et al. 2015. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 23: 950-5. PMID: 26314424
- [Effect of ADAM10 Inhibitor GI254023X on Proliferation and Apoptosis of Multiple Myeloma H929 Cells and Its Possible Mechanisms]. | Chen, LL., et al. 2015. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 23: 1628-32. PMID: 26708884
- Clostridium perfringens Delta-Toxin Damages the Mouse Small Intestine. | Seike, S., et al. 2019. Toxins (Basel). 11: PMID: 31013617
- The Cxadr-Adam10 complex plays pivotal roles in tight junction integrity and early trophoblast development in mice. | Jeong, Y., et al. 2019. Mol Reprod Dev. 86: 1628-1638. PMID: 31373105
- Inhibition of CD44 intracellular domain production suppresses bovine articular chondrocyte de-differentiation induced by excessive mechanical stress loading. | Sobue, Y., et al. 2019. Sci Rep. 9: 14901. PMID: 31624271
- Involvement of ADAM10 in acrolein-induced astrocytic inflammation. | Park, JH., et al. 2020. Toxicol Lett. 318: 44-49. PMID: 31639409
- Pharmacologic Inhibition of ADAM10 Attenuates Brain Tissue Loss, Axonal Injury and Pro-inflammatory Gene Expression Following Traumatic Brain Injury in Mice. | Appel, D., et al. 2021. Front Cell Dev Biol. 9: 661462. PMID: 33791311
- CX3CL1 Overexpression Prevents the Formation of Lung Metastases in Trastuzumab-Treated MDA-MB-453-Based Humanized Tumor Mice (HTM). | Wege, AK., et al. 2021. Cancers (Basel). 13: PMID: 34070094
Inhibitor of:
ADAM, ADAM10, ADAM19, ADAM26, ADAM7, ADAM8, ADAM9, Meprin Aβ, NET-7, and Penumbra.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GI 254023X, 1 mg | sc-490114 | 1 mg | $166.00 |