ly294002

LY294002 (SF 1101) 是一种 PI3K 的广谱抑制剂，抑制 PI3Kα、PI3Kδ 和 PI3Kβ (IC50=0.5 0.57 0.97 μM)。LY294002 也是 DNA-PK 抑制剂 (IC50=1.4 μM) 和 CK2 抑制剂 (IC50=98 nM)。LY294002 可以激活凋亡和自噬。

LY-294002 hydrochloride (NSC 697286) 是一种合成的 PI3Kα δ β 分子抑制剂（IC50：0.5 0.57 0.97 μM，在无细胞试验中）；在溶液中比 Wortmannin 更稳定，也是自噬体形成的阻断剂。

SF1126 is a relevant pan and dual first-in-class PI3K BRD4 inhibitor. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment.

LY303511 是 LY294002 的结构类似物，可增强 SHEP-1 神经母细胞瘤细胞的TRAIL 敏感性，还可逆地阻断 MIN6 胰岛瘤细胞中的K+电流，IC50为64.6±9.1 μM。

Cyclo(L-Phe-L-Val) is a metabolite of the sponge bacterium Pseudoalteromonas sp. NJ6-3-1 that can autoinduce production of antibacterial substances active against S. aureus when co-cultured at a low cell density. It induces neurite outgrowth and branching of chick cortical neurons in vitro when used at concentrations of 16 and 32 μM. It increases phosphorylation of the PI3K substrate Akt, and neurite outgrowth induced by cyclo(L-Phe-L-Val) can be blocked by the PI3K inhibitor LY294002 . Cyclo(L-Phe-L-Val) enhances axon sprouting of calcitonin gene-related protein positive (CGRP+) primary afferents in the spinal cord following crush injury and of serotonin neurons in uninjured spinal cord. Cyclo(L-Phe-L-Val) is also a bitter taste component of cocoa and roasted coffee.

LY 303511 hydrochloride 是LY294002 的一种结构类似物。LY 303511 hydrochloride 可增强 SHEP-1 神经母细胞瘤细胞的TRAIL 敏感性，还可逆地阻断 MIN6 胰岛瘤细胞中的K+电流。

Mytoxin B 是一种大环内脂，作用与 LY294002 相似，也是一种 ADC 细胞毒素 (ADC cytotoxin)。Mytoxin B 能够利用 PI3K Akt 通路，进而诱导细胞凋亡 (apoptosis)。

LY303511, a structural analog of LY294002, selectively inhibits mTOR-dependent phosphorylation of S6K, unlike its counterpart, which acts as a phosphatidylinositol 3-kinase (PI3K) inhibitor. It effectively reduces cell proliferation in human lung epithelial adenocarcinoma cells by hindering G2/M phase progression and suppressing casein kinase 2 activity. Additionally, LY303511 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitivity in HeLa cells resistant to TRAIL-induced apoptosis and blocks voltage-gated potassium (Kv) channels.