LY294002

Alias: LY-294002; LY 294002; LY294002
Cat No.:V0103 Purity: ≥98%
LY294002,a morpholine-containing compound designed based on the flavonoid quercetin,is apotent and cell-permeable PI3K inhibitor, inhibiting PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively.
LY294002 Chemical Structure CAS No.: 154447-36-6
Product category: PI3K
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
2mg
5mg
10mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of LY294002:

  • LY-294002 hydrochloride
Official Supplier of:
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Purity & Quality Control Documentation

Purity: =99.23%

Purity: ≥98%

Product Description

LY294002, a morpholine-containing compound designed based on the flavonoid quercetin, is a potent and cell-permeable PI3K inhibitor, inhibiting PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively. Additionally, it inhibits BET (for example, BRD2, BRD3, and BRD4). It is more stable in solutions than the PI3K inhibitor Wortmannin. By acting on the ATP binding site of the catalytic subunit of PI3K, LY294002 is selective against p110α, p110β, p110γ and p110δ.

Biological Activity I Assay Protocols (From Reference)
Targets
p110α (IC50 = 0.5 μM); p110δ (IC50 = 0.57 μM); p110β (IC50 = 0.97 μM); human CK2 (IC50 = 98 nM); human CK2α2 (IC50 = 3.869 μM); DNA-PK (IC50 = 1.4 μM)
ln Vitro
LY294002 is not only selective for PI3Ks; it may also act on other lipid kinases and other, seemingly unrelated proteins. Additionally to mTOR and DNA-PK, LY294002 has been demonstrated to inhibit CK2 (casein kinase 2) and Pim-1, as well as other protein kinases. Apoptosis is triggered and cell proliferation is inhibited as a result of LY294002's inactivation of Akt/PKB. In these colon cancer cell lines, LY294002 exhibits a striking growth-inhibitory and apoptosis-inducing effect, along with decreased expression of phosphorylated Akt (Ser473). [2] In tumor cells, LY294002 significantly increases nuclear pyknosis and reduces cytoplasmic volume. As a result, LY294002 significantly reduces the proliferation of ovarian cancer cells in culture. 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. The impact of LY294002 on cell cycle progression may shed light on a potential connection between the PI3K activation pathway and the control of the cancer cell cycle. [3]
ln Vivo
LY294002 exhibits remarkable effectiveness in the mouse peritonitis carcinomatosa model because it also induces apoptosis and suppresses tumor growth, particularly in LoVo tumors. [2] Ovarian carcinoma growth and ascites formation are markedly reduced by LY294002.[3] LY294002 significantly slows down the development of ascites and ovarian carcinoma.[3]
Enzyme Assay
PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1μM ATP. At room temperature (24oC), the kinase reaction lasts for an hour before being stopped by the addition of PBS. Then, IC50 values are calculated by fitting a variable slope sigmoidal dose-response curve. Kinase selectivity screening is used to determine the inhibition of CK2 and GSK3β (glycogen synthase kinase 3β). In 10μM ATP, LY294002 is evaluated against the Upstate panel of kinases.
Cell Assay
Inoculated into 96-well microtiter plates are 1.0×105 cells (100 μL volume/well). After adding LY294002, triplicate wells are cultured at 37 °C for 0 – 48 hours. Following treatment, 10 μL of Premix WST-1 is added to each microculture well, and the plates are then incubated for 60 minutes at 37 °C. At this point, an absorbance measurement at 450 nm is made using a microplate reader.
Animal Protocol
Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
0–100 mg/kg
Administered via i.p.
References

[1]. Biochem J. 2007 Jun 15;404(3):449-58.

[2]. Clin Cancer Res. 2002 Jun;8(6):1957-63.

[3]. Clin Cancer Res. 2000 Mar;6(3):880-6.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H17NO3
Molecular Weight
307.3432
Exact Mass
307.12084
Elemental Analysis
C, 74.25; H, 5.58; N, 4.56; O, 15.62
CAS #
154447-36-6
Appearance
Solid powder
SMILES
C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4
InChi Key
CZQHHVNHHHRRDU-UHFFFAOYSA-N
InChi Code
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
Chemical Name
2-morpholin-4-yl-8-phenylchromen-4-one
Synonyms
LY-294002; LY 294002; LY294002
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~36 mg/mL (117.1 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: ~21 mg/mL (~68.3 mM)
Solubility (In Vivo)
4%DMSO+30%PEG 300+5%Tween 80+ddH2O: 5mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.2537 mL 16.2686 mL 32.5373 mL
5 mM 0.6507 mL 3.2537 mL 6.5075 mL
10 mM 0.3254 mL 1.6269 mL 3.2537 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • BIO-acetoxime

    Pharmacological inhibition of GSK-3 kinase activity blunts antiviral innate immunity. Mol Cell Biol. 2015 Sep 1;35(17):3029-43.

  • BIO-acetoxime

    Absence of GSK-3 does not affect IRF3 activation.

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