LY 294002 Hydrochloride Chemical Properties

Melting point:

183-185℃

Boiling point:

494.6±45.0 °C(Predicted)

Density 

1.266

storage temp. 

Sealed in dry,Store in freezer, under -20°C

solubility 

DMSO: >5 mg/mL

form 

solid

pka

0.55±0.20(Predicted)

color 

white to off-white

Water Solubility 

Soluble in DMSO at 5mg/ml. Insoluble in water

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 4 months.

InChI

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

C1(N2CCOCC2)OC2=C(C3=CC=CC=C3)C=CC=C2C(=O)C=1

CAS DataBase Reference

154447-36-6

Safety Information

Safety Statements 

24-25

WGK Germany 

3

HS Code 

29349990

MSDS

• Language:English Provider:SigmaAldrich

LY 294002 Hydrochloride Usage And Synthesis

Description

LY294002 is a selective phosphatidylinositol 3-kinase (PI3K) inhibitor with a 2.7-fold greater potency than quercetin. LY294002 inhibits purified PI3K with an IC₅₀ of 1.4 μM.

Uses

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

Uses

A potent blocker of PI 3-kinase/Akt signaling.

Uses

LY 294002 is a Phosphatidylinositol 3-kinase (PI3K) inhibitor which has shown to block the formation of tumor tissues in bone marrow cavity an abolish multiple myeloma (MM) induced osteoclast formation and osteolysis in SCID mice.

Definition

ChEBI: LY294002 is a chromone substituted with a phenyl group at position 8 and a morpholine group at position 2. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, an autophagy inhibitor and a geroprotector. It is a member of chromones, a member of morpholines and an organochlorine compound.

Biological Activity

A highly selective inhibitor of phosphatidylinositol 3-kinase (IC 50 values are 0.31, 0.73, 1.06 and 6.60 μ M for PI3K β , PI3K α , PI3K δ and PI3K γ respectively). Inhibits proliferation and induces apoptosis in human colon cancer cells in vitro and in vivo .

target

p110α

References

[1] C. VLAHOS. A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002).[J]. The Journal of Biological Chemistry, 1994, 93 1: 5241-5248. DOI:10.1016/s0021-9258(17)37680-9.
[2] SEVERINE I GHARBI. Exploring the specificity of the PI3K family inhibitor LY294002.[J]. ACS Applied Energy Materials, 2007: 15-21. DOI:10.1042/BJ20061489.
[3] SANCHEZMARGALET V. Role of Phosphatidylinositol-3-Kinase in Insulin Receptor Signaling: Studies with Inhibitor, LY294002[J]. Biochemical and biophysical research communications, 1994, 204 2: Pages 446-452. DOI:10.1006/bbrc.1994.2480.

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