Cat. No.: HY-19956

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GI254023X

(Synonyms: GI4023; SRI028594)

21 Cited Publications

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Based on 21 publication(s) in Google Scholar

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC₅₀s of 2.5 and 5.3 nM, respectively.

For research use only. We do not sell to patients.

Purity: 99.60%
CAS No.: 260264-93-5
Formula: C₂₁H₃₃N₃O₄
Molecular Weight:391.50

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GI254023X Chemical Structure

CAS No.: 260264-93-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (21)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC₅₀s of 2.5 and 5.3 nM, respectively.

IC₅₀ & Target

IC50: 2.5 nM (MMP9), 5.3 nM (ADAM10)^[1]

All MMP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
KM-H2	IC₅₀	10 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA	[PMID: 26871660]
KM-H2	IC₅₀	10 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA	[PMID: 26871660]
KM-H2	IC₅₀	10 μM Compound: GIX; GI254023X	Inhibition of ADAM-17 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA Inhibition of ADAM-17 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA	[PMID: 26871660]
KM-H2	IC₅₀	12 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human KM-H2 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA	[PMID: 26871660]
L-428	IC₅₀	10 μM Compound: GIX; GI254023X	Inhibition of ADAM-17 in human L428 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA Inhibition of ADAM-17 in human L428 cells assessed as reduction in pervanadate-induced soluble ALCAM shedding after 24 hrs by ELISA	[PMID: 26871660]
L-428	IC₅₀	12 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA	[PMID: 26871660]
L-428	IC₅₀	15 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA	[PMID: 26871660]
L-428	IC₅₀	5 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human L428 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA	[PMID: 26871660]
L-540	IC₅₀	10 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble ULBP3 shedding after 24 hrs by ELISA	[PMID: 26871660]
L-540	IC₅₀	12 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced soluble MICB shedding after 24 hrs by ELISA	[PMID: 26871660]
L-540	IC₅₀	7 μM Compound: GIX; GI254023X	Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA Inhibition of ADAM-10 in human L540 cells assessed as reduction in pervanadate-induced TNFalpha shedding after 24 hrs by ELISA	[PMID: 26871660]

In Vitro

In cellular assay 25 μM and even a concentration of 1 μM GI254023X strongly reduces constitutive RAGE shedding; 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 ADAM protease inhibitors (e.g GI254023x). A2780 cells are incubated with the ADAM-10/ADAM-17 inhibitor TAPI-2, as well as the ADAM-10-selective inhibitor GI254023x, as the level of expressed ADAM-10 is on average 9.8-fold higher on mRNA level compare with ADAM-17. 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 260264-93-5
Appearance Solid
Molecular Weight 391.50
Formula C₂₁H₃₃N₃O₄
Color White to off-white
SMILES

O=C(N[C@H](C(NC)=O)C(C)(C)C)[C@@H]([C@@H](N(C=O)O)C)CCCC1=CC=CC=C1
Synonyms

GI4023; SRI028594
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (21)

All Cell Imaging/StainingWBFlow CytometryRT-PCR

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Journal Impact Factor

Signal Transduct Target Ther

Human adipose and umbilical cord mesenchymal stem cell-derived extracellular vesicles mitigate photoaging via TIMP1/Notch1. [Abstract]

2024 Oct 30;9(1):294. PMID: 39472581

GI254023X purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Oct 30;9(1):294. [Abstract]

Luciferase-reporter assays of HES1 transcriptional activity in HDFs after UVB, FM (culture medium), EV, TIMP1, GI254023X (10 μM), and VPA treatment. After UVB, HDFs were incubated with ADAM10 inhibitor GI254023X for 2 h, and then cells were incubated with fibroblast medium for an additional 24 h.
Cell

Cell-autonomous control of CAR signaling and receptor shedding via ADAM17-mediated proteolysis. [Abstract]

2026 Jun 25;189(13):3883-3902.e23. PMID: 42143019
Neuron

Differential and substrate-specific inhibition of γ-secretase by the C-terminal region of ApoE2, ApoE3, and ApoE4. [Abstract]

2023 Jun 21;111(12):1898-1913.e5. PMID: 37040764
Adv Sci (Weinh)

Overcoming the Tumor Collagen Barriers: A Multistage Drug Delivery Strategy for DDR1-Mediated Resistant Colorectal Cancer Therapy. [Abstract]

2024 Jul 2:e2402107. PMID: 38953306

GI254023X purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jul 2:e2402107. [Abstract]

Immunoblotting analysis of proteins extracted from MC38 cells, which were plated on CAFs‐derived ECM and pre‐stimulated with collagen I (20 µg/mL) for 18 h followed by treatment with CPT‐11 (20 µM) for 48 h alone, or along with inhibitor, GI254023X (20 µM) for 24 h.
Cell Rep Med

DDX5 super-enhancer promotes vasculogenic mimicry formation and metastasis in nasopharyngeal carcinoma by enhancing ADAM10 transcription. [Abstract]

2025 Jun 17;6(6):102146. PMID: 40412383
J Exp Med

Host factor TIMP1 sustains long-lasting myeloid-biased hematopoiesis after severe infection. [Abstract]

2023 Dec 4;220(12):e20230018. PMID: 37851372

GI254023X purchased from MedChemExpress. Usage Cited in: J Exp Med. 2023 Dec 4;220(12):e20230018. [Abstract]

Treatment scheme and representative FACS plots showing percentages of CD11b+ myeloid cells and B cells in the BM of GI254023X (100 mg/kg, ip, 7 days)-treated mice (n = 9) or vehicle-treated mice (n = 7).

GI254023X purchased from MedChemExpress. Usage Cited in: J Exp Med. 2023 Dec 4;220(12):e20230018. [Abstract]

Hes1 expression in human HSPCs. Human CD34+ HSPCs were cultured in medium with indicated stimuli for 5 h. Expression of Hes1 transcripts was determined by qRT-PCR. Induction fold of Hes1 is calculated as the ratio of Hes1 levels stimulated with DLL4 plus GI254023X (1 μM, 5 h) or TIMP1 to that with DLL4 alone. Symbols depict data from three independent experiments. * P < 0.05; ns, P > 0.05 (unpaired two-tailed Student’s t test). RU, relative unit.
Cancer Lett

Direct interaction of platelet with tumor cell aggravates hepatocellular carcinoma metastasis by activating TLR4/ADAM10/CX3cl1 axis. [Abstract]

2024 Mar 31:585:216674. PMID: 38280480
Genes Dis

Sulfuretin exerts diversified functions in the processing of amyloid precursor protein. [Abstract]

2020 Nov 21;8(6):867-881. PMID: 34522714

GI254023X purchased from MedChemExpress. Usage Cited in: Genes Dis. 2020 Nov 21;8(6):867-881. [Abstract]

Representative Western blots of CTF proteins in SH-SY5Y-APP cells pretreated with vehicle (DMSO), β-secretases inhibitor (LY2811376, 50 μM) or α-secretases inhibitor (GI254023X, 10 μM) in combination with DAPT (250 nM) for 1 h, then incubated with or without sulfuretin at 20 μM for 24 h.
Mucosal Immunol

Neutrophil ADAM10 promotes migration and inflammation in ARDS by modulating adhesion and chemokine signaling. [Abstract]

2025 Sep 12:S1933-0219(25)00093-5. PMID: 40947020
Elife

Synaptotagmin 7 is targeted to the axonal plasma membrane through γ-secretase processing to promote synaptic vesicle docking in mouse hippocampal neurons. [Abstract]

2021 Sep 20;10:e67261. PMID: 34543184
Respir Res

B1 cells drive pulmonary emphysema progression through ADAM10. [Abstract]

2026 Mar 31;27(1):205. PMID: 41917947
Invest Ophthalmol Vis Sci

Inhibitor of DNA-Binding 3 Is a Novel Regulator of Limbal Epithelial Cell Migration Via the EphA2/Akt Signaling Pathway. [Abstract]

2025 Jul 1;66(9):2. PMID: 40590805
Philos Trans R Soc Lond B Biol Sci

Alpha-secretase inhibition impairs Group I metabotropic glutamate receptor-mediated protein synthesis, long-term potentiation and long-term depression. [Abstract]

2024 Jul 29;379(1906):20230481. PMID: 38853546
Front Aging Neurosci

Nasal Delivery of D-Penicillamine Hydrogel Upregulates a Disintegrin and Metalloprotease 10 Expression via Melatonin Receptor 1 in Alzheimer's Disease Models. [Abstract]

2021 Apr 15;13:660249. PMID: 33935689
Mediators Inflamm

miR-23b Negatively Regulates Sepsis-Induced Inflammatory Responses by Targeting ADAM10 in Human THP-1 Monocytes. [Abstract]

2019 Oct 31;2019:5306541. PMID: 31780861
Sci Rep

Chronic inflammation promotes gastric cancer progression via ADAM10-mediated cleavage of CX3CL1. [Abstract]

2026 Feb 15;16(1):9169. PMID: 41691064
J Cancer

ADAM10 is a key player in the diagnosis, prognosis and metastasis of non-small cell lung cancer (NSCLC). [Abstract]

2025 Feb 11;16(5):1736-1746. PMID: 39991567
Traffic

AP2S1 regulates APP degradation through late endosome-lysosome fusion in cells and APP/PS1 mice. [Abstract]

2023 Jan;24(1):20-33. PMID: 36412210
Brain Hemorrhages

Erratum regarding previously published articles. [Abstract]

2022 Dec;3(4):218. PMID: 36406202
bioRxiv

2025 Sep 21.
Research Square Preprint

2023 Nov 20.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (255.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5543 mL

12.7714 mL

25.5428 mL

5 mM

0.5109 mL

2.5543 mL

5.1086 mL

10 mM

0.2554 mL

1.2771 mL

2.5543 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[3]

Cell death is quantified based on plasma membrane permeabilization. When apply the ADAM10 (a-secretase) inhibitor GI254023X (5 mM), slices are cultured in serum-/glucose-free medium for 48 h containing the inhibitor or its respective carrier (DMSO) as control. Round circles of identical size (Ø 500mm) are positioned in equivalent locations within the CA1 region of each hippocampus image and all PI-stained cells are counted using 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Verena V. Metz, et al. Induction of RAGE Shedding by Activation of G Protein-Coupled Receptors. PLoS One. 2012. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5543 mL	12.7714 mL	25.5428 mL	63.8570 mL
	5 mM	0.5109 mL	2.5543 mL	5.1086 mL	12.7714 mL
	10 mM	0.2554 mL	1.2771 mL	2.5543 mL	6.3857 mL
	15 mM	0.1703 mL	0.8514 mL	1.7029 mL	4.2571 mL
	20 mM	0.1277 mL	0.6386 mL	1.2771 mL	3.1928 mL
	25 mM	0.1022 mL	0.5109 mL	1.0217 mL	2.5543 mL
	30 mM	0.0851 mL	0.4257 mL	0.8514 mL	2.1286 mL
	40 mM	0.0639 mL	0.3193 mL	0.6386 mL	1.5964 mL
	50 mM	0.0511 mL	0.2554 mL	0.5109 mL	1.2771 mL
	60 mM	0.0426 mL	0.2129 mL	0.4257 mL	1.0643 mL
	80 mM	0.0319 mL	0.1596 mL	0.3193 mL	0.7982 mL
	100 mM	0.0255 mL	0.1277 mL	0.2554 mL	0.6386 mL

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GI254023X

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Protease Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GI254023X

All MMP Isoforms

Biological Activity

Chemical Information

Publications (21)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GI254023X

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Protease Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GI254023X

All MMP Isoforms

Biological Activity

Chemical Information

Publications (21)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GI254023X Related Classifications

HY-19956 Related Classifications