LY294002

For research purposes only

Cat. No BA142114777

Availability Please, check stock availability.

Description of biological activity

Phosphatidylinositol 3-Kinase (PI3K) inhibitor. The compound inhibits PI3K with IC50 1.4 μM. It exhibits a very broad specificity profile, inhibiting the class I PI3Ks, PI3KC2b, PI3KC2c, mTOR, casein kinase 2, and DNA-PK all with IC50 values in the low micromolar range [2]. Within the class I PI3Ks, LY294002 exhibits a maximum of approximately 10-fold selectivity between any two isoforms, with p110b being most sensitive (2.9 μM) and p110c the least sensitive (38 μM)
IC50: 1.4 μM (PI3K) [1]
Target: Phosphatidylinositol 3-Kinase (PI3K)

TECHNICAL INFORMATION

2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one Phosphatidylinositol 3-Kinase (PI3K) inhibitor.

IUPAC Name: 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one

CAS Number: 154447-36-6

Purity: > 98% chemical purity (LCMS)

1H-NMR spectrum (click to enlarge)

REFERENCES

1. Bioorg. Med. Chem. Lett., В 2006,В 16,В 969 - 973
2. J. Biol.Chem. 1994, 269, 5241-8
3. J.Med.Chem. 2005, 48, 569-585

Latest added compounds

5-(4-Hydroxy-4-methyl-isoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-(3-methyl-5-trifluoromethyl-1H-pyrazol-4-ylmethyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione

Selective inhibitor of MCT1 with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. Both lactate transport and cell growth are potently inhibited.

Anti-cancer

Inhibitors

 
5-(4-chlorophenyl)-N-{[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl}pyridine-3-carboxamide

selective inhibitor of Nav1.8 sodium channel (IC50 = 3 nM); for TRPV1, P2X2/3, Cav2.2 calcium channels, KCNQ2/3 potassium channels IC50 >10 µM

Analgesic

Inhibitors

 
1-[4-chloro-3-(trifluoromethyl)benzenesulfonyl]-4-[4-(5-methyl-1H-pyrazol-1-yl)benzoyl]piperazine

inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smuf1)

Bone disorders

Inhibitors