1. Metabolic Enzyme/Protease
  2. MMP
  3. GI254023X

GI254023X (Synonyms: GI4023; SRI028594)

Cat. No.: HY-19956 Purity: 99.67%
Handling Instructions

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.

GI254023X Chemical Structure

GI254023X Chemical Structure

CAS No. : 260264-93-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 191 In-stock
Estimated Time of Arrival: December 31
1 mg USD 144 In-stock
Estimated Time of Arrival: December 31
5 mg USD 222 In-stock
Estimated Time of Arrival: December 31
10 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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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]

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].

Molecular Weight

391.50

Formula

C₂₁H₃₃N₃O₄

CAS No.

260264-93-5

SMILES

O=C(N[[email protected]](C(NC)=O)C(C)(C)C)[[email protected]@H]([[email protected]@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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (255.43 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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

Purity: 99.67%

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Keywords:

GI254023XGI4023SRI028594GI 4023GI-4023SRI 028594SRI-028594MMPMatrix metalloproteinasesInhibitorinhibitorinhibit

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GI254023X
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