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Chemical Structure| 260264-93-5 Chemical Structure| 260264-93-5

Structure of GI254023X
CAS No.: 260264-93-5

Chemical Structure| 260264-93-5

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GI 254023X is a potent and selective ADAM10 metalloproteinase inhibitor.

Synonyms: SRI028594; GI4023

4.5 *For Research Use Only !

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Product Details of GI254023X

CAS No. :260264-93-5
Formula : C21H33N3O4
M.W : 391.50
SMILES Code : O=C(N[C@@H](C(C)(C)C)C(NC)=O)[C@@H]([C@@H](N(O)C=O)C)CCCC1=CC=CC=C1
Synonyms :
SRI028594; GI4023
MDL No. :MFCD19381832
InChI Key :GHVMTHKJUAOZJP-CGTJXYLNSA-N
Pubchem ID :9952396

Safety of GI254023X

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Murine mesothelioma PM27 cells 5 µM 16 h To evaluate the effect of GI254023X on migration and invasion of PM27 cells. Results showed that GI254023X significantly reduced the migratory and invasive abilities of PM27 cells. PMC6756017
Murine mesothelioma AB12 cells 5 µM 16 h To evaluate the effect of GI254023X on migration and invasion of AB12 cells. Results showed that GI254023X significantly reduced the migratory and invasive abilities of AB12 cells. PMC6756017
DU145 cells 50 μM 24 h Inhibited ADAM10 activity, reduced the release of ephrin-A5, thereby suppressing the proliferation, migration, and invasion of prostate cancer cells. PMC9098485
Mouse hippocampal neurons 1 µM From DIV6 to DIV14 GI254023X treatment restored the loss of mushroom dendritic spines and increased the number of excitatory synapses in R6/2 hippocampal neurons. PMC11335257

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice AKT/c-Myc-driven HCC model Intraperitoneal injection 20 mg/kg From day 10 to day 24 Evaluate the inhibitory effect of ADAM10 inhibitor GI254023X on tumor progression PMC11384939
C57BL/6N mice Controlled cortical impact (CCI) model Intraperitoneal injection 100 mg/kg 30 min and 24 h after trauma GI254023X treatment attenuates brain tissue loss, axonal injury and pro-inflammatory gene expression. PMC8005610

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.26mL

12.77mL

2.55mL

1.28mL

25.54mL

5.11mL

2.55mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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