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Chemical Structure| 1346547-00-9 Chemical Structure| 1346547-00-9

Structure of GSK583
CAS No.: 1346547-00-9

Chemical Structure| 1346547-00-9

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GSK583 is a selective inhibitor of RIP2 Kinase and IC50 value is 5 nM.

Synonyms: GSK583

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Product Details of GSK583

CAS No. :1346547-00-9
Formula : C20H19FN4O2S
M.W : 398.45
SMILES Code : FC1=CC2=C(NN=C2NC3=CC=NC4=CC=C(S(=O)(C(C)(C)C)=O)C=C34)C=C1
Synonyms :
GSK583
MDL No. :MFCD30343846
InChI Key :XLOGLWKOHPIJLV-UHFFFAOYSA-N
Pubchem ID :67469084

Safety of GSK583

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

Related Pathways of GSK583

pyroptosis

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
U251 cells 1 μM GSK583 pretreatment inhibited the up-regulation of CD133 and SOX-2 protein expression induced by RIP2 overexpression PMC9627370
BV2 cells 20 μM 24 hours To evaluate the inhibitory effect of GSK583 on RIP2, the results showed that GSK583 significantly inhibited RIP2 expression. PMC7708246

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice U251 cell xenograft model Oral 50 mg/kg/day Once daily for 7 days GSK583 combined with TMZ enhanced the cytotoxic effect of TMZ on RIP2-overexpressing U251 cells and inhibited tumor growth PMC9627370
Rat Acute MDP-driven peritonitis model Oral 50 mg/kg/d Once daily for 6 weeks Evaluate the efficacy of GSK583 in an inflammation model, showing that its blood concentration remained above its human whole blood IC50 value for 24 hours, indicating good efficacy PMC6187414
C57BL/6 mice Collagenase-induced intracerebral hemorrhage model Intraventricular injection 3 mg/kg Once daily for 3 weeks To evaluate the effect of GSK583 on brain injury induced by intracerebral hemorrhage, the results showed that GSK583 significantly alleviated brain damage. PMC7708246
C57BL/6J mice Acute HDM asthma model Chow 2 mg/kg Single dose Early inhibition of RIP2 was sufficient to reduce lung pathology, including inflammation, mucus production, and collagen deposition, and to reduce Th2 and Th17 immune responses. PMC7895314

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.55mL

2.51mL

1.25mL

25.10mL

5.02mL

2.51mL

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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