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LY 303511

MCE 国际站：LY 303511

品牌：MedChemExpress (MCE)

货号：HY-15643

CAS 号：154447-38-8

生物活性：LY303511是LY294002的结构类似物。LY303511不抑制PI3K。LY303511增强SHEP-1神经母细胞瘤细胞对TRAIL的敏感性。LY303511可逆性地阻断MIN6胰岛瘤细胞中的K+电流（IC50=64.6±9.1 μM）。

体外研究(In Vitro)：LY303511 is structurally identical to LY294002 except for a substitution of -O for -NH in the morpholine ring, and does not potently inhibit PI3K. Treatment of cells with LY303511 causes an increase in calcein spread similar to levels of LY294002. The ability of LY303511 to increase gap junctional intercellular communication (GJIC) does not occur concomitant with inhibition of phosphorylation of AKT as measured by immunoblotting[1]. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via H2O2-MAPK activation and up-regulation of death receptors. SHEP-1 cells are exposed to varying concentrations of LY303511 (LY30), TRAIL, and a combination of the two (1 h preincubation with LY303511 followed by TRAIL for 4 hours). SHEP-1 cells are responsive to TRAIL (~10%, ~15%, and ~30% reduction in the surviving fraction at 25, 50, and 100 ng/mL, respectively); however, treatment with LY303511 (12.5, 25, or 50 μM) has no effect on cell viability. However, incubation of cells with LY303511 (25 μM) for 1 hour followed by 4 hours exposure to 50 ng/mL of TRAIL has a strong synergistic effect (~40% reduction in viable cells with LY303511+TRAIL versus ~15% with TRAIL alone)[2]. LY303511 is a negative control compound with respect to PI3K activity. In MIN6 insulinoma cells, Wortmannin (100 nM) has no effect on whole-cell outward K+ currents, but LY294002 and LY303511 reversibly block currents in a dose-dependent manner (IC50=9.0±0.7 μM and 64.6±9.1 μM, respectively). Kv2.1 and Kv1.4 are highly expressed in beta-cells, and in Kv2.1-transfected tsA201 cells, 50 μM LY294002 and 100 μM LY303511 reversibly inhibit currents by 99% and 41%, respectively. LY303511 blocks currents with an IC50 of 64.6±9.1 µM, with a maximal inhibition of ~90% at 500 µM (n≥5 cells at each concentration)[3]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：Intraperitoneal administration of vehicle or LY303511 (10 mg/kg/day) is performed when tumors reach a volume of ~150 mm3, at which time 35 mice have developed a tumor. After 21 days, >15% of the mice require euthanasia because of excessive tumor growth, and these data are censored due to unreliable estimates of average tumor volume. The administration of LY303511, 10 mg/kg/day, is sufficient to inhibit PC-3 tumor growth in vivo[4]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：306.36

Formula：C19H18N2O2

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：请按照分析证书中推荐的条件储存产品。

Cell Assay [2]：人神经母细胞瘤SHEP-1细胞培养于添加10%胎牛血清和1%青霉素的DMEM培养基中。在典型的细胞存活率测定中，将SHEP-1细胞（每孔8×10⁴个）接种于24孔板中培养24小时后，分别暴露于LY303511（12.5、25和50 μM）、TRAIL（25、50和100 ng/mL）以及二者联合处理（先用LY303511预孵育1小时，再用TRAIL孵育4小时）。采用结晶紫染色法测定细胞毒性。药物处理后，用PBS洗涤细胞，并用200 μL结晶紫溶液孵育20分钟。用蒸馏水洗去多余的结晶紫溶液，剩余的结晶用20%乙酸溶解。使用自动酶联免疫吸附测定仪（ELISA）在 595 nm 波长处测定吸光度来确定细胞活力。细胞活力实验采用类似方法进行，分别加入 2000 单位/mL 的过氧化氢酶、4 μM 的 JNK 抑制剂 SP600125、10 μM 的 p38 抑制剂 SB202190、20 μM 的 MAPK/ERK 激酶 (MEK) 抑制剂 PD98059、50 μM 的 caspase-8 抑制剂 Z-IETD-FMK 或泛 caspase 抑制剂 Z-VAD-FMK，或死亡受体阻断抗体（4 μg/mL 抗 DR4 或 1 μg/mL 抗 DR5），或在转染了用于分别沉默 JNK 和 ERK 表达的小干扰 RNA (siRNA) 的细胞中进行。在加入 TRAIL 之前，细胞先与 LY303511 和相应的抑制剂或过氧化氢酶预孵育 1 小时。 LY303511 对 TRAIL 诱导的细胞凋亡具有类似的敏化作用，在 SY5Y 神经母细胞瘤、T98G 胶质母细胞瘤、Jurkat 白血病、CEM 骨髓性白血病、HeLa 卵巢癌和 HT29 结直肠癌细胞系中均表现出类似的敏化作用[2]。 MCE 尚未独立确认这些方法的准确性。仅供参考。

Animal Administration [4]：Mice[4] Human prostate adenocarcinoma (PC-3) cells (ATCC CRL-1435) are cultured in vitro before harvesting and implantation of 1×106 cells in 20% Matrigel per athymic NCR nude mouse by subcutaneous injection at the flank. Inoculated mice are subdivided into four groups of 10. Administration of vehicle or LY303511, 10 mg/kg/day, is begun (day 1) when tumors reach ~150 mm3 (n=35), and tumor volumes are measured for 30 days at the indicated time points. MCE尚未独立确认这些方法的准确性。 仅供参考。

文献引用：MCE 顾客使用本产品发表 5 篇科研文献

提供质量检测报告：Data Sheet、产品使用指南

产品活性：LY303511 是 LY294002 的一种结构类似物，但 LY303511 不抑制 PI3K。LY303511 可增强 SHEP-1 神经母细胞瘤细胞的TRAIL 敏感性。LY303511 可逆地阻断 MIN6 胰岛瘤细胞中的 K+ 电流 (IC50=64.6±9.1 μM)。

IC50 & Target：TRAIL[2] IC50: 64.6±9.1 µM (K+ currents, in MIN6 insulinoma cells)[3]

相关产品：LY 303511 hydrochloride  | Repaglinide  | E-4031  | E-4031 (Standard)  | Repaglinide (Standard)  | NS309  | Zefamenib  | GW9508  | GW9508 (Standard)  | NS6180  | APD668  | CVN293

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客户发表文献：
[1]. Nature. 2026 Sep;657(8131):549-558.
[2]. Nature. 2026 Sep;657(8132):755-764.
[3]. Nature. 2026 Sep;657(8133):1027-1034.
[4]. Nature. 2026 Sep;657(8131):477-486.
[5].Nature. 2026 Sep;657(8132):789-799.
[6]. Nature. 2026 Sep;657(8131):517-524.
[7]. Nature. 2026 Sep;657(8133):1045-1052.
[8]. Cell. 2026 Sep 14:S0092-8674(26)01003-2.
[9]. Cell. 2026 Sep 3;189(18):5688-5705.e13.
[10]. Cell. 2026 Sep 2:S0092-8674(26)00937-2.

参考文献：
[1]. Bodenstine TM, et al. Homotypic gap junctional communication associated with metastasis suppression increases with PKA activity and is unaffected by PI3K inhibition. Cancer Res. 2010 Dec 1;70(23):10002-11.
[2]. El-Kholy W, Macdonald PE, Lin JH, The phosphatidylinositol 3-kinase inhibitor LY294002 potently blocks K(V) currents via a direct mechanism. FASEB J. 2003 Apr;17(6):720-2.
[3]. Shenoy K, et al. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via hydrogen peroxide-mediated mitogen-activated protein kinase activation and up-regulation of death receptors. Cancer Res. 2009 Mar 1;69(5):1941-50.
[4]. Kristof AS, et al. LY303511 (2-piperazinyl-8-phenyl-4H-1-benzopyran-4-one) acts via phosphatidylinositol 3-kinase-independent pathways to inhibit cell proliferation via mammalian target of rapamycin (mTOR)- and non-mTOR-dependent mechanisms. J Pharmacol E