GI254023X [260264-93-5]
Cat# HY-19956-1mg
Size : 1mg
Brand : MedChemExpress
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
CAS No. : 260264-93-5
This product is a controlled substance and not for sale in your territory.
Based on 12 publication(s) in Google Scholar
View All MMP Isoform Specific Products:
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] |
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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. |
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Molecular Weight |
391.50 |
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Formula |
C21H33N3O4 |
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CAS No. |
260264-93-5 |
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Appearance |
Solid |
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Color |
White to off-white |
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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 |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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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
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.
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 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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.
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Purity & Documentation |
Purity: 99.67% |
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References |
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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.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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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
- Metabolic Enzyme/Protease
- MMP