LY294002

SKU: orb1306761

特色

描述

LY294002

研究领域

Cell Biology, Stem Cell & Developmental Biology

图片与验证

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关键属性

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CAS 号	154447-36-6
MW	307.34
纯度	>98%
分子式	C₁₉H₁₇NO₃
SMILES	O=c1cc(oc2c(cccc12)-c1ccccc1)N1CCOCC1
靶点	Kinase
溶解性	Soluble in DMSO (up to 25 mg/ml).

生物活性

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靶点 IC50	p110δ:0.57 μM (cell free)\|DNA-PK:1.4 μM (cell free)\|p110α:0.5 μM (cell free)\|CK2 (human):98 nM\|p110β:0.97 μM (cell free)\|PI3K:1.4 μM\|PI3K:1.6 μM (Ki)\|RBL-2H3 cell:5 μM\|CK2α2 (human):3.869 μM
体内	METHODS: To detect anti-tumor activity in vivo, LY294002 (25 mg/kg twice weekly) and cisplatin (5 mg/kg once weekly) were intraperitoneally injected into BALB/C nu/nu mice harboring human pancreatic cancer tumor AsPC-1 for three weeks. RESULTS: Tumor volume increased in the control mice, while the cisplatin or LY294002 treatment groups showed a 77% and 70% reduction in tumor volume, respectively. The combination treatment group was more effective, with tumor volume growth decreasing to 44% of the control group's volume. METHODS: To investigate whether pharmacological blockade of PI3K could ameliorate the development of LPS-induced acute liver injury in mice, LY294002 (40 μM; 10 μL) was administered by single intraperitoneal injection to the LPS-induced acute hepatic injury BALB/c mouse model. RESULTS: In LPS-induced hepatitis, LY294002 treatment markedly inhibited the intrahepatic synthesis of various disease-associated pro-inflammatory cytokines, including tumor necrosis factor-α, IL-6, IL-1β, and INF-γ. Significant inhibition of IκB phosphorylation was observed in liver samples from LPS-injured mice with LY294002. Therefore, LY294002 may protect the liver from LPS-induced injury by inhibiting the IκB nuclear factor κ light chain enhancer of the activated B cell-dependent signaling pathway.
体外	METHODS: Human pancreatic cancer cells AsPC-1, BxPC-3 and PANC-1 were treated with LY294002 (5-45 µM) for 24 h. Cell growth inhibition was detected by MTT. RESULTS: LY294002 dose-dependently induced the growth of AsPC-1, BxPC-3 and PANC-1 cells with IC50 of 40 μM, 5 μM and 35 μM, respectively. METHODS: Chinese hamster ovary cells CHO-IR expressing human insulin receptor were treated with LY294002 (5 µM) for 5 min and stimulated with Insulin (1 nM, 10 min), and the expression levels of target proteins were detected by Western Blot. RESULTS: LY294002 blocked insulin-induced phosphorylation of PKB Ser473 in CHO-I R cells. METHODS: Human nasopharyngeal carcinoma cells CNE-2Z were treated with LY294002 (10-75 μmol/L) for 24-48 h. Apoptosis was detected by Flow Cytometry. RESULTS: LY294002 dose-dependently induced apoptosis in CNE-2Z cells.
细胞研究	The cells were seeded into 96-well plates at 5000 cells/well. Twenty-four hours after cells were seeded, the medium was removed and replaced in the presence of LY294002 (0 μmol/L, 10 μmol/L, 25 μmol/L, 50 μmol/L, and 75 μmol/L) dissolved in DMSO or DMSO only for an additional 24 h and 48 h. To avoid any nonspecific toxic effects of DMSO on cell growth, DMSO concentrations were maintained at 0.5% in all experiments. MTT dye (5 mg/mL) was added to each well. The reaction was stopped by the addition of DMSO, and optical density was measured at 490 nm on a multiwell plate reader. Background absorbance of the medium in the absence of cells was subtracted. All samples were assayed in triplicate, and the mean for each experiment was calculated. Results were expressed as a percentage of control, which was considered to be 100% .
动物研究	Athymic nude mice were used when they were 6-8 weeks. Mice were randomly divided into free separated into five groups (n = 4 mice). Mice were housed in the same environment with controlled temperature, humidity, and a 12 h light/dark cycle. Mice were inoculated subcutaneously with CNE-2Z cells (1 × 10^6 cells/mouse in 200 μl of RPMI-1640) into the flank. The tumor take rate was 100%. After 1 week, an intraperitoneal injection was performed to the xenograft mice with different dosage of LY294002 (10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg twice weekly (n = 4 mice), each group for 4 weeks. Treated mice have monitored any signs. Body weight and tumors size were measured twice a week. Tumor size was measured using calipers and tumor volume was calculated (volume = long axis × short axis^2). At the end of the treatment, all mice were euthanized. One part of tumor tissue was fixed in formalin and embedded in paraffin, and another part was stored at -70°C .

储存与操作

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储存	RT
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Autophagy, Apoptosis, broad-spectrum, CaseinKinase, Casein Kinase, carcinoma, DNA-dependent protein kinase, DNAPK, DNA-PK, CNE-2Z, Inhibitor, Human, Leptin, inhibit, NPC, Lysophosphatidic acid, LY294002, LY-294002, LY 294002, NSC 697286, nasopharyngeal, nuclear, NSC697286, NSC-697286, spermatozoa, reversibly, YAP, p110δ, p110β, p110α, SF1101, SF-1101, SF 1101, Phosphoinositide 3-kinase, PI3K, translocation, tumor

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纯度：
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MW:
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可选规格： 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 ml x 10 mM (in DMSO)
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SF1126 [orb1706641]
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PI-828 [orb1706792]
纯度：
99.95% (May vary between batches)
CAS 号：
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MW:
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可选规格： 5 mg, 25 mg, 1 mg, 10 mg, 50 mg, 100 mg, 1 ml x 10 mM (in DMSO), 200 mg

质量保证

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化合物标识

PubChem CID

3973 ↗

关键属性

−

暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	99.98% (May vary between batches)
CAS 号：	934389-88-5
MW:	343.81
分子式：	C₁₉H₁₇NO₃·HCl

CAS 号：	105049-15-8
MW:	528.59
分子式：	C₂₉H₃₆O₉

纯度：	99.91% (May vary between batches)
CAS 号：	154447-38-8
MW:	306.36
分子式：	C₁₉H₁₈N₂O₂

CAS 号：	936487-67-1
MW:	852.84
分子式：	C₃₉H₄₈N₈O₁₄

纯度：	99.95% (May vary between batches)
CAS 号：	942289-87-4
MW:	322.36
分子式：	C₁₉H₁₈N₂O₃

LY294002

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

LY-294002 hydrochloride [orb1303185]

Mytoxin B [orb1686325]

LY 303511 [orb1703203]

SF1126 [orb1706641]

PI-828 [orb1706792]

质量保证

化合物标识

关键属性

实验方案信息

可选规格