Home Immunology & Inflammation Immunology & Inflammation related inhibitor GI254023X For research use only.

GI254023X

Synonyms: GI 4023, SRI028594

GI254023X (GI 4023, SRI028594) 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.GI254023X can inhibit MMP9.

GI254023X Chemical Structure

GI254023X Chemical Structure

CAS No. 260264-93-5

Purity & Quality Control

GI254023X Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
L428 Function assay 24 hrs Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA, IC50=5μM. 26871660
L540 Function assay 24 hrs Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA, IC50=7μM. 26871660
KM-H2 Function assay 24 hrs Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA, IC50=10μM. 26871660
KM-H2 Function assay 24 hrs Inhibition of ADAM-17 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA, IC50=10μM. 26871660
KM-H2 Function assay 24 hrs Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA, IC50=10μM. 26871660
L428 Function assay 24 hrs Inhibition of ADAM-17 in human L428 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA, IC50=10μM. 26871660
L540 Function assay 24 hrs Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA, IC50=10μM. 26871660
KM-H2 Function assay 24 hrs Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA, IC50=12μM. 26871660
L428 Function assay 24 hrs Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA, IC50=12μM. 26871660
L540 Function assay 24 hrs Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA, IC50=12μM. 26871660
L428 Function assay 24 hrs Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA, IC50=15μM. 26871660
Click to View More Cell Line Experimental Data

Biological Activity

Description GI254023X (GI 4023, SRI028594) 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.GI254023X can inhibit MMP9.
Targets
ADAM10 [1]
(Cell-free assay)
5.3 nM
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models BALB/c mice
Dosages 200 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 391.50 Formula

C21H33N3O4
CAS No. 260264-93-5 SDF --
Smiles CC(C(CCCC1=CC=CC=C1)C(=O)NC(C(=O)NC)C(C)(C)C)N(C=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 79 mg/mL ( (201.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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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