LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC₅₀分别为 0.5μM/0.57 μM/0.97μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。
        LY294002是选择性的, 可渗透细胞的特定PI3K抑制剂，可作用于酶的ATP结合位点，且抑制自体吞噬的螯合作用。在体内，LY294002也抑制肿瘤生长和诱导凋亡，尤其作用于LoVo肿瘤, 因此作用于鼠癌性腹膜炎模型具有明显药效。 LY294002明显抑制卵巢癌生长和腹水形成。

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

NSC 697286; SF 1101; LY 294002; LY-294002

white to off-white powder

DMSO：36 mg/mL (117.13 mM)
Ethanol：21 mg/mL (68.32 mM)

p110α,p110δ,p110β,DNA-PK

LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. LY294002 is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. 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 effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation.

LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma.

[1] Chaussade C, et al. Biochem J, 2007, 404(3), 449-58.
[2] Semba S, et al. Clin Cancer Res, 2002, 8(6), 1957-63.
[3] Hu L, et al. Clin Cancer Res, 2000, 6(3), 880-6.