Catalog No.S8660 Synonyms: GI 4023
Molecular Weight(MW): 391.50
GI254023X is a selective inhibitor of ADAM10 with 100-fold selectivity for ADAM10 over ADAM17. The IC50 values for recombinant ADAM10 amd ADAM17 are 5.3 nM and 541 nM, respectively.
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|Description||GI254023X is a selective inhibitor of ADAM10 with 100-fold selectivity for ADAM10 over ADAM17. The IC50 values for recombinant ADAM10 amd ADAM17 are 5.3 nM and 541 nM, respectively.|
In cell-based cleavage experiments GI254023X potently blocks the constitutive release of IL6R, CX3CL1 and CXCL16, which is in line with the reported involvement of ADAM10 but not ADAM17 in this process. By contrast, the compound does not affect the PMA-induced shedding. In addition to ADAM10 and ADAM17, GI254023X is a moderate inhibitor of ADAM9 with an IC50 of 280 nM.
Acute treatment with GI254023X in an AD mouse model substantially reduces brain LRP1 shedding and increases Aβ40 levels in the plasma, indicating enhanced Aβ transit from the brain to the periphery. Furthermore, both soluble and insoluble Aβ40 and Aβ42 brain levels are decreased following GI254023X treatment, but these effects lack statistical significance.
-  Herzog C, et al. J Biol Chem. 2014, 289(19):13308-22.
-  Ludwig A, et al. Comb Chem High Throughput Screen. 2005, 8(2):161-71.
-  Schmidt S, et al. J Exp Med. 2018, 215(4):1205-1225.
|In vitro||DMSO||78 mg/mL (199.23 mM)|
|Ethanol||78 mg/mL (199.23 mM)|
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