LY 294002

Product NameLY 294002
CAS934389-88-5
MFC19H18ClNO3
MW343.80412
EINECS
MOL File934389-88-5.mol

Chemical Properties

storage temp.	2-8°C
solubility	DMSO: >5mg/mL
form	solid
color	white to off-white
biological source	microbial (Staphylococcus roseus)
InChI	1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2
InChIKey	CZQHHVNHHHRRDU-UHFFFAOYSA-N
SMILES	O=C1C=C(Oc2c1cccc2-c3ccccc3)N4CCOCC4

Safety Information

WGK Germany	3
HS Code	29349990
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

LY 294002 Hydrochloride is a highly selective inhibitor of Phosphatidylinositol 3-kinase (PI3K). It is a salt analogue of LY 294002 (L486590).

General Description

LY-294,002 hydrochloride is a derivative of the flavonoid, quercetin and elicits higher inhibition on the enzyme phosphoinositide 3-kinase (PI3K). LY-294,002 inhibits nuclear factor kappa B signaling in macrophages. It elevates expression of autophagosomal protein LC3 and promotes apoptosis in gastric and nasopharyngeal cancer cells. LY-294,002 modulates action potential repolarization and improves myocyte contractility.

Biological Activity

Specific cell permeable phosphatidylinositol 3-kinase inhibitor.

in vivo

LY294002 hydrochloride (10, 25, 50, 75 mg/kg; i.p.; twice weekly; for 4 weeks) significantly reduces mean NPC tumor burden in a dose-dependent manner. LY294002 (10, 25 mg/kg) is less effective in decreasing tumor burden^[4].
LY294002 hydrochloride (1.2 mg/kg per day; i.p.; for 14 days) prevents Leptin (60 ug/kg)-induced adverse effects on spermatozoa in Sprague-Dawley rats^[5].

Animal Model:	Athymic nude mice (6-8 weeks) with CNE-2Z xenograft^[4]
Dosage:	10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg
Administration:	IP; twice weekly, for 4 weeks
Result:	Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner.

IC 50

CK2: 0.098 μM (IC₅₀); CK2α2: 3.869 μM (IC₅₀)

storage

Room temperature