GI254023X (Synonyms: GI4023; SRI028594)

Name: GI254023X
Brand: MedChemExpress
SKU: HY-19956
Rating: 5.0 (19 reviews)

Cat. No.: HY-19956 Purity: 99.60%: Data Sheet
COA

SDS
Handling Instructions
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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.

CAS No. : 260264-93-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 19 publication(s) in Google Scholar

19 Publications Citing Use of MCE GI254023X

Cell Imaging/Staining

Flow Cytometry

RT-PCR

: 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.

: 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.

: 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.

: 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.

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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]

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 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-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-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.

Molecular Weight

391.50

Formula

C₂₁H₃₃N₃O₄

CAS No.

260264-93-5

Appearance

Solid

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (279 KB) SDS (396 KB)

COA (251 KB) LCMS (366 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]

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].

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

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]

Complete Stock Solution Preparation Table

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

GI254023X Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GI254023X260264-93-5GI4023 SRI028594GI 4023GI-4023SRI028594SRI 028594SRI-028594MMPMatrix metalloproteinasesInhibitorinhibitorinhibit

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GI254023X (Synonyms: GI4023; SRI028594)

Customer Review

GI254023X Related Antibodies

19 Publications Citing Use of MCE GI254023X

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GI254023X Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GI254023X Related Classifications

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