化合物 LY2409881 trihydrochloride|T2081|TargetMol

LY2409881 trihydrochloride
946518-60-1

￥283 1mg 起订

￥395 2mg 起订

￥662 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 LY2409881 trihydrochloride

英文名称：: LY2409881 trihydrochloride

CAS号：: 946518-60-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥95%

产品类别：: 抑制剂

货号：: T2081

Product Introduction

Bioactivity

名称	LY2409881 trihydrochloride
描述	LY2409881 trihydrochloride is a novel specific inhibitor of IKK2 (IC50: 30 nM); IC50 for IKK1 and other common kinases is at least one log higher.
细胞实验	Cytotoxicity is evaluated using the CellTiter-Glo Reagent according to the manufacturer's manual. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment relative to the untreated control from the same experiment. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software.(Only for Reference)
激酶实验	CYP3A activity is assessed using the probe reactions, midazolam-1′-hydroxylation and testosterone 6β-hydroxylation. For reversible inhibition, incubations (37°C, 10 min) are composed of (final concentrations): potassium phosphate buffer (100 mM, pH 7.4), β-NADPH (1 mM), magnesium chloride (5 mM), microsomal protein (0.025 mg/mL), probe substrate (1 μM midazolam or 25 μM testosterone), LCL161 (0, 0.5, 1, 5, 10, 25, 50, or 100 μM) and organic solvent (0.2% acetonitrile for midazolam, 0.2% methanol for testosterone). After a 3-minute preincubation, the reactions are initiated by addition of β-NADPH and terminated by addition of acetonitrile (two volumes). Reactions are previously shown to be linear with respect to time and protein concentration (results not shown) with midazolam and testosterone turnover of 8.7±1.3% (n=3) and 2.6±0.20%, respectively. Formation of 1′-hydroxymidazolam and 6β-hydroxytestosterone is determined by LC-MS/MS as described below[3].
体外活性	在SCID-beige移植瘤小鼠模型中,LY2409881（50/100/200 mg/kg,i.p.）可显著抑制肿瘤生长.
体内活性	LY240988对卵巢癌SKOV3细胞株具有中等毒性。在弥漫性大B细胞淋巴瘤细胞中,LY2409881对激活的NF-?B有抑制作用,浓度和时间依赖性地抑制细胞生长并使细胞凋亡。在SUDHL2细胞中,LY2409881可协同环磷酰胺和阿霉素抑制细胞生长,但对LY1细胞无协同效果。在SUDHL22和LY1细胞中,组蛋白去乙酰化酶抑制剂罗米地辛与LY2409881可协同抑制细胞生长。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 16 mg/mL (26.9 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	LY 2409881 \| LY2409881 trihydrochloride \| LY-2409881 Trihydrochloride \| LY2409881 Trihydrochloride \| Inhibitor \| IκB kinase \| Apoptosis \| IKK \| LY-2409881 \| inhibit \| I kappa B kinase \| LY-2409881 trihydrochloride \| LY 2409881 Trihydrochloride
相关产品	L-Glutamic acid \| Metronidazole \| 5-Fluorouracil \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Tributyrin \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Salicylic acid \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 抗乳腺癌化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| HIF-1化合物库 \| 抗卵巢癌化合物库 \| NF-κB 通路分子库 \| 抗前列腺癌化合物库

LY2409881|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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