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GI254023X

Catalog No. T7522 CAS 260264-93-5

Synonyms: GI 254023X

GI254023X is a potent MMP9 and ADAM10 inhibitor (IC50s: 2.5 and 5.3 nM) with 100-fold selectivity for the α-secretase ADAM10 over ADAM17 (TACE). GI254023X can remarkably inhibit the proliferation and induce the apoptosis of H929 cells. Its mechanism may be associated with inbihition of Notch1 activation.

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GI254023X, CAS 260264-93-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
2 mg	In stock	$ 143.00
5 mg	In stock	$ 182.00
10 mg	In stock	$ 247.00
25 mg	In stock	$ 478.00
50 mg	In stock	$ 715.00
100 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 196.00

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Purity: 98.56%

Purity: 98.21%

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Storage & Solubility Information

Description	GI254023X is a potent MMP9 and ADAM10 inhibitor (IC50s: 2.5 and 5.3 nM) with 100-fold selectivity for the α-secretase ADAM10 over ADAM17 (TACE). GI254023X can remarkably inhibit the proliferation and induce the apoptosis of H929 cells. Its mechanism may be associated with inbihition of Notch1 activation.
Targets&IC50	MMP9:2.5 nM (cell free), ADAM10:5.3 nM (cell free)
In vitro	In the cellular assay, GI254023X (1-25 μM) strongly reduces constitutive RAGE shedding and also PACAP-inducing shedding of RAGE is significantly reduced. At a concentration of 100 nM, a slight inhibition of RAGE shedding is still observed. In in vitro assays with recombinant proteinases, GI254023X discriminates between ADAM17 (IC50: 541 nM) and ADAM10 (IC50: 5.3 nM)/MMP9 (IC50: 2.5 nM) [1]. CXCL16 shedding is inhibited by GI254023x. A2780 cells are incubated with the ADAM-10/ADAM-17 inhibitor TAPI-2, as well as the ADAM10-selective inhibitor GI254023x, as the level of expressed ADAM10, is on average 9.8-fold higher on mRNA level compare with ADAM17. In addition, GI254023x also prevents CXCL16 shedding from the cell membrane and is even more potent than TAPI-2[2]. When apply the specific ADAM10 (α-secretase) inhibitor GI254023X (5 mM) to serum/glucose-deprived slices, PI counts are significantly increased in comparison with DMSO (carrier)-treated controls [3].
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 [4].
Cell Research	Cell death is quantified based on plasma membrane permeabilization. When applying the ADAM10 (a-secretase) inhibitor GI254023X (5 mM), slices are cultured in the serum-/glucose-free medium for 48 h containing the inhibitor or its respective carrier (DMSO) as control. Round circles of identical size (? 500mm) are positioned in equivalent locations within the CA1 region of each hippocampus image and all PI-stained cells are counted using the software. Cell viability assays are performed with a commercial kit according to the manufacturer's instructions. The assay quantitates ATP levels, an indicator of metabolically active cells, photometrically with a fluorescence plate reader. Additionally, the live-dead cell staining kit are applied according to the manual. Cells are simultaneously stained with green fluorescent calcein-AM (4mM; ex/em: 495/515 nm) to detect intracellular esterase activity (viable cells) and red fluorescent ethidium homodimer-3 (2mM; ex/em: 530/635 nm) to indicate loss of plasma membrane integrity (dead cells) [3].

Synonyms	GI 254023X
Molecular Weight	391.5
Formula	C21H33N3O4
CAS No.	260264-93-5

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (255.43 mM), Sonication is recommended.

References and Literature

1. Verena V. Metz, et al. Induction of RAGE Shedding by Activation of G Protein-Coupled Receptors. PLoS One. 2012. 2. M J M Gooden, et al. Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity. British Journal of Cancer (2014) 110, 1535–1544. 3. N Milosch, et al. Holo-APP and G-protein-mediated signaling are required for sAPPa-induced activation of the Akt. Cell Death Dis. 2014 Aug 28;5:e1391. 4. Shackleton B, et al. Inhibition of ADAM10 promotes the clearance of Aβ across the BBB by reducing LRP1 ectodomain shedding. Fluids Barriers CNS. 2016 Aug 8;13(1):14.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Angiogenesis related Compound Library Anti-Fibrosis Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Wnt/Hedgehog/Notch Compound Library Anti-Aging Compound Library Anti-Cancer Compound Library Immunology/Inflammation Compound Library

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Keywords

GI254023X 260264-93-5 Immunology/Inflammation Proteases/Proteasome MMP Immunology/Inflammation related SRI 028594 SRI028594 GI 4023 inhibit GI-254023X Matrix metalloproteinases GI 254023X SRI-028594 Inhibitor GI4023 GI-4023 inhibitor

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