LY 294002
LY 294002 Basic information
- Product Name:
- LY 294002
- Synonyms:
-
- LY 294002, Hydrochloride Salt, >99%
- LY 294002, HYDROCHLORIDE SALT
- LY-294,002 hydrochloride, 98%, selective inhibitor of PI 3-kinase
- LY-294,002 hydrochloride, ≥98% (HPLC)
- 2-morpholin-4-yl-8-phenylchromen-4-one,hydrochloride
- 2-morpholino-8-phenyl-4H-chromen-4-one hydrochloride
- LY-294002 hydrochloride, 10 mM in DMSO
- LY-294,002 hydrochloride【L9908】
- CAS:
- 934389-88-5
- MF:
- C19H18ClNO3
- MW:
- 343.80412
- Mol File:
- 934389-88-5.mol
LY 294002 Chemical Properties
- storage temp.
- 2-8°C
- solubility
- DMSO: >5mg/mL
- form
- solid
- color
- white to off-white
- biological source
- microbial (Staphylococcus roseus)
LY 294002 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
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