LY294002 (HCl Salt)
2-(4-MORPHOLINO)-8-PHENYL-4H-1-BENZOPYRAN-4-ON
CAS: 154447-36-6
Molecular Formula: C19H17NO3
LY294002 (HCl Salt) - Names and Identifiers
LY294002 (HCl Salt) - Physico-chemical Properties
| Molecular Formula | C19H17NO3 |
| Molar Mass | 307.34 |
| Density | 1.266 |
| Melting Point | 183-185℃ |
| Boling Point | 494.6±45.0 °C(Predicted) |
| Water Solubility | Soluble in DMSO at 5mg/ml. Insoluble in water |
| Solubility | Soluble in DMSO (25 mg/ml warm), ethanol (25 mg/ml warm), chloroform, water (< 50 ug/m |
| Appearance | Pale yellow solid |
| Color | white to off-white |
| pKa | 0.55±0.20(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 4 months. |
| In vitro study | LY294002 is a non-specific inhibitor that, in addition to class I PI3Ks, also inhibits other types of PI3Ks, mTOR, DNA-PK and other protein kinases, such as CK2 and Pim-1. LY294002 inactivates Akt/PKB, thereby inhibiting cell proliferation and inducing apoptosis. LY294002 acts on colon cancer cell lines to decrease the expression of phosphorylated Akt (Ser473), significantly inhibit growth and induce apoptosis. LY294002 acts on tumor cells, inducing obvious nuclear condensation and reducing cytoplasmic volume. Thus, LY294002 significantly inhibited ovarian cancer cell proliferation in vitro. LY294002 induced cells to stop in G1 phase, resulting in almost all melanoma cell proliferation was inhibited, and some MG-63 (Osteosarcoma cell line) proliferation was inhibited. The effect of LY294002 on the cell cycle can be used to study the relationship between PI3K activation pathway and cancer cell cycle. |
| In vivo study | In vivo, LY294002 also inhibits tumor growth and induces apoptosis, especially in LoVo tumors, and thus has significant efficacy in the mouse model of cancerous peritonitis. LY294002 significantly inhibited ovarian cancer growth and ascites formation. |
LY294002 (HCl Salt) - Risk and Safety
| Safety Description | S24 - Avoid contact with skin. S25 - Avoid contact with eyes. |
| WGK Germany | 3 |
| HS Code | 29349990 |
LY294002 (HCl Salt) - Reference
| Reference Show more | 1. [IF=5.037] Lei Zhang et al."3-Epipachysamine B suppresses proliferation and induces apoptosis of breast cancer cell via PI3K/AKT/mTOR signaling pathway."Life Sci. 2021 Nov;285:119995 2. [IF=4.36] Pin Gong et al."Hypoglycemic effect of astragaloside IV via modulating gut microbiota and regulating AMPK/SIRT1 and PI3K/AKT pathway."J Ethnopharmacol. 2021 Dec;281:114558 3. [IF=4.207] Jianghua Ding et al."LPCAT1 promotes gefitinib resistance via upregulation of the EGFR/PI3K/AKT signaling pathway in lung adenocarcinoma."J Cancer. 2022; 13(6): 1837–1847 |
LY294002 (HCl Salt) - Reference Information
| Use | LY294002/PI3K inhibitors have been shown to block the formation of tumor tissue in the bone marrow cavity in SCID mice and eliminate osteoclast formation and osteolysis caused by multiple myeloma (MM). ly294002 is a phosphatidylinositol 3 kinase (PI3K) inhibitor, which can block the formation of tumor tissue in bone marrow cavity and eliminate the formation of osteoclasts and osteolysis induced by multiple myeloma (MM) in SCID mice. |
| biological activity | LY294002 (SF 1101, NSC 697286) is the first small molecule that is known to inhibit PI3Kα/δ/β. In cell-free determination, IC50 is 0.5 μM/0.57 μM/0.97 μM respectively. It is more stable in solution than in Wortmannin and can also block the formation of autophagosomes. It can not only bind class I PI3Ks and other PI3K-related kinases, but also some novel targets unrelated to the PI3K family. LY294002 can inhibit CK2, and the corresponding IC50 value is 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and can activate autophagy and apoptosis. |
| target | TargetValue CK2 (cell-free say) 98 nM p110α (cell-free say) 0.5 μM p110δ (cell-free say) 0.57 μM p110β (cell-free say) 0.97 μM DNA-PK (cell-free) 1.4 μM |
| Target | Value |
| CK2 (Cell-free assay) | 98 nM |
| p110α (Cell-free assay) | 0.5 μM |
| p110δ (Cell-free assay) | 0.57 μM |
| p110β (Cell-free assay) | 0.97 μM |
| DNA-PK (Cell-free) | 1.4 μM |
| in vitro research | LY294002 is a non-specific inhibitor. in addition to class I PI3Ks, it can also inhibit other types of PI3Ks, mTOR, DNA-PK and other protein kinases, such as CK2 and Pim-1. LY294002 inactivates Akt/PKB, thus inhibiting cell proliferation and inducing cell apoptosis. LY294002 acts on colon cancer cell lines to reduce the expression of phosphorylated Akt (Ser473), significantly inhibit growth and induce apoptosis. LY294002 acts on tumor cells to induce obvious nuclear pyknosis and reduce cytoplasmic volume. Therefore, in vitro, LY294002 significantly inhibited the proliferation of ovarian cancer cells. LY294002 induced cells to stop in G1 phase, resulting in almost all melanoma cell proliferation inhibited and some MG-63 (osteosarcoma cell line) proliferation inhibited. The effect of LY294002 on cell cycle can be used to study the relationship between PI3K activation pathway and cancer cell cycle. |
| in vivo study | in vivo, LY294002 also inhibit tumor growth and induce apoptosis, especially on LoVo tumor, so it has obvious drug effect on mouse cancerous peritonitis model. LY294002 significantly inhibited ovarian cancer growth and ascites formation. |
Last Update：2024-04-09 20:45:29
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