GI254023X

Catalog No.S8660 Synonyms: GI 4023

GI254023X Chemical Structure

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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Biological Activity

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.
Targets
ADAM10 [1]
(Cell-free assay)
5.3 nM
In vitro

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[2]. In addition to ADAM10 and ADAM17, GI254023X is a moderate inhibitor of ADAM9 with an IC50 of 280 nM[1].

In vivo

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[5].

Protocol

Cell Research:

[3]

+ Expand
  • Cell lines: HCA-7 cells
  • Concentrations: 3 μM
  • Incubation Time: 24 h
  • Method:

    HCA-7 cells are treated for 24 h with 0.1% DMSO, the metalloprotease inhibitors GI (GI254023X, ADAM10-selective, 3 µM) and GW (GW280264X, ADAM10- and ADAM17-selective, 3 µM), the pan-metalloprotease inhibitor Marimastat (MM; 10 µM), and the EGF-R kinase inhibitor AG1478 (10 µM). Cells stimulated with 100 ng/ml EGF served as positive control. Tyrosine-phosphorylated EGF-R and total EGF-R are assessed by Western blot analysis.


    (Only for Reference)
Animal Research:

[4]

+ Expand
  • Animal Models: BALB/c mice
  • Formulation: DMSO
  • Dosages: 200 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.23 mM)
Ethanol 78 mg/mL (199.23 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 391.50
Formula

C21H33N3O4

CAS No. 260264-93-5
Storage powder
in solvent
Synonyms GI 4023

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID