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LY-294002 hydrochloride

🥰Excellent
Catalog No. T4079Cas No. 934389-88-5
Alias LY294002 hydrochloride, LY 294002 hydrochloride

LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.

LY-294002 hydrochloride

LY-294002 hydrochloride

🥰Excellent
Purity: 99.95%
Catalog No. T4079Alias LY294002 hydrochloride, LY 294002 hydrochlorideCas No. 934389-88-5
LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.
Pack SizePriceAvailabilityQuantity
1 mg$37In Stock
2 mg$50In Stock
5 mg$68In Stock
10 mg$98In Stock
25 mg$179In Stock
50 mg$298In Stock
100 mg$471In Stock
1 mL x 10 mM (in DMSO)$68In Stock
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Purity:99.95%
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Product Introduction

Bioactivity
Description
LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.
Targets&IC50
PI3Kδ:0.57μM, PI3Kβ:0.97 μM, PI3Kα:0.5μM
In vitro
LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. In these colon cancer cell lines, LY294002 shows a remarkable growth-inhibitory and apoptosis-inducing effect and decreases expression of phosphorylated Akt (Ser473)[2]. LY294002 induces diminished cytoplasmic volume and obvious nuclear pyknosis in the tumor cells. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation[3].
In vivo
LY294002 can suppress tumor growth and induce apoptosis, especially in the LoVo tumors. Thus, It shows remarkable effectiveness in the mouse peritonitis carcinoma tosa model [2]. LY294002 markedly inhibits growth and ascites formation of ovarian carcinoma [3].
Kinase Assay
PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose-response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition are established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.[4]
Cell Research
Cell lines: Colon cancer cell lines DLD-1,LoVo,HCT15,and Colo205. Concentrations: 0–50 μM. Incubation Time: 0–48 hours. Method: 1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates.LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours.After treatment,Premix WST-1 (10 μL) is added to each microculture well,and the plates are incubated for 60 minutes at 37oC,after which absorbance at 450 nm is measured with a microplate reader.[2]
Animal Research
Animal Models: Two groups of athymic nude mice (5–7 weeks) are inoculated i.p.with OVCAR-3 cells. Formulation: Dissolved in DMSO plus 0.25 ml of PBS. Dosages: 0–100 mg/kg. Administration: i.p.[3]
AliasLY294002 hydrochloride, LY 294002 hydrochloride
Chemical Properties
Molecular Weight343.81
FormulaC19H17NO3·HCl
Cas No.934389-88-5
SmilesCl.O=c1cc(oc2c(cccc12)-c1ccccc1)N1CCOCC1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (145.43 mM)
Ethanol: 5 mM
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.9086 mL14.5429 mL29.0858 mL145.4292 mL
5 mM0.5817 mL2.9086 mL5.8172 mL29.0858 mL
DMSO
1mg5mg10mg50mg
10 mM0.2909 mL1.4543 mL2.9086 mL14.5429 mL
20 mM0.1454 mL0.7271 mL1.4543 mL7.2715 mL
50 mM0.0582 mL0.2909 mL0.5817 mL2.9086 mL
100 mM0.0291 mL0.1454 mL0.2909 mL1.4543 mL

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