AS-252424

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

Structure Search

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-

HIDE SMILES / InChI

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16789742/ https://www.ncbi.nlm.nih.gov/pubmed/28713374

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
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 5 Target ID: P48736 Gene ID: 5294.0 Gene Symbol: PIK3CG Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/16789742	Inhibitor 8297		30.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Unknown 2578

PubMed

Title	Date	PubMed
		252160134

Patents

Sample Use Guides

In Vivo Use Guide

Unknown

Route of Administration: Unknown

In Vitro Use Guide

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 `Sat Dec 16 10:04:47 GMT 2023` Edited by `admin` on `Sat Dec 16 10:04:47 GMT 2023`
Record UNII	63D4RUV1GN
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AS-252424

Common Name

English

2,4-THIAZOLIDINEDIONE, 5-((5-(4-FLUORO-2-HYDROXYPHENYL)-2-FURANYL)METHYLENE)-, (5Z)-

Systematic Name

English

Code System Code Type Description

PUBCHEM

11630874