LY-294002 hydrochloride | CAS# 934389-88-5 | Prototypical PI 3-kinase inhibitor

MedKoo Cat#: 574773 | Name: LY-294002 hydrochloride

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LY-294002 hydrochloride is a PI 3-, CK2-, mTOR-, PLK1-, PIM1- and PIM3-kinase inhibitor. LY-294002 hydrochloride inhibits proliferation and induces apoptosis in human colon cancer cells and suppresses proliferation of mESCs.

Chemical Structure

LY-294002 hydrochloride

CAS#934389-88-5 (HCl)

Theoretical Analysis

MedKoo Cat#: 574773

Name: LY-294002 hydrochloride

CAS#: 934389-88-5 (HCl)

Chemical Formula: C19H18ClNO3

Exact Mass: 343.0975

Molecular Weight: 343.81

Elemental Analysis: C, 66.38; H, 5.28; Cl, 10.31; N, 4.07; O, 13.96

Price and Availability

Size	Price	Availability
5mg	USD 300.00	2 Weeks
10mg	USD 550.00	2 Weeks
25mg	USD 950.00	2 Weeks

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Related CAS #

154447-36-6 (free base) 934389-88-5 (HCl)

Synonym

LY-294002 hydrochloride; LY294002 hydrochloride; LY 294002 hydrochloride; LY-294002 HCl; LY294002 HCl; LY 294002 HCl

IUPAC/Chemical Name

2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one hydrochloride

InChi Key

OQZQSRICUOWBLW-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H17NO3.ClH/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;1H

SMILES Code

O=C1C=C(N2CCOCC2)OC3=C(C4=CC=CC=C4)C=CC=C13.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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.

In vitro activity:

The inhibitory effect of LY294002 on proliferation of multiple myeloma cell U266 was explored. U266 cell viability was reduced in time- and dose-dependent manner after treatment with 5, 10, 20 µmol/L of LY294002 for 24, 48, 72 h. The 5, 10, 20 µmol/L LY294002 leaded to cell nucleus dense and thick, and the cell cycle arrested in the G1 phase (P<0.01). The expressions of BCL-2, Cyclin D1, Cyclin E, PI3K and p-AKT were down-regulated (P<0.01), and the expression of BAX up-regulated (P<0.01). These results indicate that LY294002 can inhibit U266 cell proliferation via suppresion of activation of PI3K/AKT signal pathway. Reference: Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2017 Aug;25(4):1092-1096. https://pubmed.ncbi.nlm.nih.gov/28823274/

In vivo activity:

The effects of LY294002 on Tourette syndrome (TS) in rats were evaluated. TS model was induced in rats by DOI (the selective 5-HT2A/2C agonist 1- (2, 5- dimethoxy -4 - iodophenyl) -2- aminopropane). Behavior was assessed by stereotypic score and autonomic activity. Inflammatory cytokines such as interleukin-6 (IL-6), interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) in serum and striatum were detected. The protein levels of PI3K/Akt/NF-B in striatum were detected by Western Blot. LY294002 treatment significantly reduced IL-6, IL-1β and TNF-α in serum and striatum of TS rats, Also, highly expressed P-PI3K, P-Akt, P-NF-κBp65, P-IκBα in TS rats were restored respectively by LY294002 treatment as indicted in western blot analysis and immunohistochemistry analysis. Thus, it was supposed that the protective effect of LY294002 against TS in rat might be associated with the regulation of PI3K/Akt/NF-B pathway. Reference: Metab Brain Dis. 2017 Oct;32(5):1619-1625. https://link.springer.com/article/10.1007%2Fs11011-017-0051-z

	Solvent	mg/mL	mM
Solubility
	DMSO	8.6	25.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 343.81 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Wang YQ, Lin Y, Zhao JD, Yang YT. [Inhibitory Effect of LY294002 on Proliferation of Multiple Myeloma Cells and Its Mechanism]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2017 Aug;25(4):1092-1096. Chinese. doi: 10.7534/j.issn.1009-2137.2017.04.023. PMID: 28823274. 2. Chen P, Wen X, Wang B, Hou D, Zou H, Yuan Q, Yang H, Xie J, Huang H. PI3K/Akt inhibitor LY294002 potentiates homoharringtonine antimyeloma activity in myeloma cells adhered to stromal cells and in SCID mouse xenograft. Ann Hematol. 2018 May;97(5):865-875. doi: 10.1007/s00277-018-3247-3. Epub 2018 Feb 15. PMID: 29450644. 3. Hongyan L, Chunyan W, Yue'e Y. LY294002, a PI3K inhibitor, attenuates Tourette syndrome in rats. Metab Brain Dis. 2017 Oct;32(5):1619-1625. doi: 10.1007/s11011-017-0051-z. Epub 2017 Jun 18. PMID: 28624893.

In vitro protocol:

In vivo protocol:

1. Hongyan L, Chunyan W, Yue'e Y. LY294002, a PI3K inhibitor, attenuates Tourette syndrome in rats. Metab Brain Dis. 2017 Oct;32(5):1619-1625. doi: 10.1007/s11011-017-0051-z. Epub 2017 Jun 18. PMID: 28624893. 2. Chen P, Wen X, Wang B, Hou D, Zou H, Yuan Q, Yang H, Xie J, Huang H. PI3K/Akt inhibitor LY294002 potentiates homoharringtonine antimyeloma activity in myeloma cells adhered to stromal cells and in SCID mouse xenograft. Ann Hematol. 2018 May;97(5):865-875. doi: 10.1007/s00277-018-3247-3. Epub 2018 Feb 15. PMID: 29450644.

1. Vlahos et al (1994) A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY 294002). J.Biol.Chem. 269 5241 PMID: 8106507 2. Blommaart et al (1997) The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes. Eur.J.Biochem. 243 240 PMID: 9030745 3. Lianguzova et al (2007) Phosphoinositide 3-kinase inhibitor LY294002 but not serum withdrawal suppresses proliferation of murine embryonic stem cells. Cell Biol.Int. 31 330 PMID: 17321171 4. Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214