Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C14H8FNO4S |
| Molecular Weight | 305.281 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC1=CC(F)=CC=C1C2=CC=C(O2)\C=C3/SC(=O)NC3=O
InChI
InChIKey=OYYVWNDMOQPMGE-SDQBBNPISA-N
InChI=1S/C14H8FNO4S/c15-7-1-3-9(10(17)5-7)11-4-2-8(20-11)6-12-13(18)16-14(19)21-12/h1-6,17H,(H,16,18,19)/b12-6-
| Molecular Formula | C14H8FNO4S |
| Molecular Weight | 305.281 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
AS-252424 is a potent and selective PI 3-kinase p110γ inhibitor. It is known, that the p110γ isoform has partially overlapping roles with p110δ in B cell development, but little is known about its role in B cell function. Recently was found, that the AS-252424 had no significant impact on B cell responses.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P48736 Gene ID: 5294.0 Gene Symbol: PIK3CG Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/16789742 |
30.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28713374
To test the effects of p110γ inhibition, was used AS-252424 compound with a biochemical IC50 = 30 nM for p110γ. Separate cultures were treated with the p110γ inhibitor AS-252424 or its diluent control (0.1% EtOH). MK-2206, an AKT inhibitor, which also reduces AKT S473 phosphorylation, was also used as a control to show ERK1/2 phosphorylation is independent of AKT activity. The p110δ inhibitor, IPI-3063, was very potent in reducing p-AKT (significant effect at 1 nM) while the p110γ inhibitor, AS-252424, had no significant effect on p-AKT signaling. IPI-3063 also reduced p-ERK1/2 with a significant effect at 10 nM, whereas AS-252424 had no significant effect.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 23:00:39 GMT 2025
by
admin
on
Mon Mar 31 23:00:39 GMT 2025
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| Record UNII |
63D4RUV1GN
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| Record Status |
Validated (UNII)
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| Record Version |
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63D4RUV1GN
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1138220-19-5
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DTXSID801017365
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900515-16-4
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