LY-294,002 hydrochloride

Modify Date: 2024-01-11 17:44:07

LY-294,002 hydrochloride Structure
LY-294,002 hydrochloride structure
Common Name LY-294,002 hydrochloride
CAS Number 934389-88-5 Molecular Weight 343.80400
Density N/A Boiling Point N/A
Molecular Formula C19H18ClNO3 Melting Point N/A
MSDS Chinese USA Flash Point N/A

 Use of LY-294,002 hydrochloride


LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research[1][2][3].

 Names

Name 2-morpholin-4-yl-8-phenylchromen-4-one,hydrochloride
Synonym More Synonyms

 LY-294,002 hydrochloride Biological Activity

Description LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research[1][2][3].
Related Catalog
Target

CK2:0.098 μM (IC50)

CK2α2:3.869 μM (IC50)

In Vitro LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion[4]. LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent[4]. LY294002 hydrochloride (10-75 μM) significantly decreases p-Akt (S473) expression levels and up-regulates caspase-9 activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration[4]. LY294002 hydrochloride (5, 10, 100 µM; for 2 hours) treatment partially suppresses Lysophosphatidic acid (LPA)-induced (20 µM; for 4 hours) nuclear translocation of YAP, accompanied by a reduction in p-AKT levels[6]. Cell Proliferation Assay Cell Line: CNE-2Z cells[4] Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Time: 24 hours and 48 hours Result: Decreased CNE-2Z cells in a dose-dependent fashion. Apoptosis Analysis Cell Line: CNE-2Z cells[4] Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Time: 24 hours and 48 hours Result: Induced apoptosis rate in a dose-dependent manner. Western Blot Analysis Cell Line: CNE-2Z cells[4] Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM Incubation Time: 24 hours and 48 hours Result: Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated caspase-9 activity in CNE-2Z cells in treated group.
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.
References

[1]. Bai R, et al. The effect of PI3K inhibitor LY294002 and gemcitabine hydrochloride combined with ionizing radiation on the formation of vasculogenic mimicry of Panc-1 cells in vitro and in vivo. Neoplasma. 2016;63(1):80-92.

[2]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58.

[3]. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21.

[4]. Jiang H, et al. Phosphatidylinositol 3-kinase inhibitor(LY294002) induces apoptosis of human nasopharyngeal carcinoma invitro and in vivo. J Exp Clin Cancer Res. 2010 Apr 22;29:34.

[5]. Md Mokhtar AH, et al. LY294002, a PI3K pathway inhibitor, prevents leptin-induced adverse effects on spermatozoa in Sprague-Dawley rats. Andrologia. 2019 Apr;51(3):e13196.

[6]. Yi-Jen Hsueh, et al. Lysophosphatidic acid induces YAP-promoted proliferation of human corneal endothelial cells via PI3K and ROCK pathways. Mol Ther Methods Clin Dev. 2015 Apr 29;2:15014.

 Chemical & Physical Properties

Molecular Formula C19H18ClNO3
Molecular Weight 343.80400
Exact Mass 343.09800
PSA 42.68000
LogP 4.16360
Storage condition 2-8°C

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport

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 Synonyms

LY-294,002 hydrochloride