化合物 BI-D1870|T6171|TargetMol

BI-D1870
501437-28-1

￥389 1mg 起订

￥563 2mg 起订

￥955 5mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 化合物 BI-D1870

英文名称：: BI-D1870

CAS号：: 501437-28-1

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：: 99.43%

产品类别：: 抑制剂

货号：: T6171

Product Introduction

Bioactivity

名称	BI-D1870
描述	BI-D1870 is a highly specific, blood-brain-permeable, and ATP-competitive inhibitor of the N-terminal AGC kinase domain of RSK, with IC50 values of 31 nM, 24 nM, 18 nM, and 15 nM for RSK1, RSK2, RSK3, and RSK4.
细胞实验	The rat embryo fibroblast cell line, Rat-2 cells were cultured on 10 cm-diameter dishes in Dulbecco's Modified Eagle's medium supplemented with 10% (v/v) FBS. HEK-293 cells were cultured on 10 cm-diameter dishes in Dulbecco's Modified Eagle's medium supplemented with 10% FBS and 1×antimycotic/antibiotic solution. Prior to stimulation, cells were cultured in the absence of serum for 16 h. Inhibitors were dissolved in DMSO at a 1000-fold higher concentration than they were used at. These inhibitors, or the equivalent volume of DMSO as a control, were added to the tissue culture medium 30 min prior to stimulation unless indicated otherwise. The final concentration of DMSO in the culture medium was 0.1% and had no effect on agonist-induced activation or phosphorylation of any of the substrates examined. The cells were stimulated with the indicated agonists and lysed in 1 ml of ice-cold Lysis Buffer and centrifuged at 16000 g at 4 °C for 5 min. The supernatants were frozen in liquid nitrogen and stored at ?80 °C until use. Protein concentrations were determined using the Bradford method with BSA as the standard [1].
激酶实验	Purified His6–RSK1, His6–RSK2 or GST–RSK21–389:S381E (1–2 units/ml) were assayed for 10 min at 30 °C in a 50 μl assay mixture in Buffer A containing 30 μM substrate peptide (KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK), 10 mM magnesium acetate and 100 μM of [γ-32P]ATP. Reactions were terminated and analyzed as described previously. The amount of enzyme that catalyzed the phosphorylation of 1 nmol of substrate peptide in 1 min was termed one unit. In order to assay RSK and MSK1 in HEK-293 or Rat-2 cell lysates, these kinases were immunoprecipitated from the cell lysates (0.1 mg of lysate protein for RSK and 0.3 mg for MSK1) and assayed as described previously, except that for RSK assays the immunoprecipitates were washed twice with Buffer A containing 1 mM ATP and twice with Buffer A prior to the assay, as a precaution to ensure dissociation of BI-D1870 from the RSK isoforms [1].
动物实验	Myelin oligodendrocyte glycoprotein (MOG) peptide 35–55. (MEVGWYRSPFSRVVHLYRNGK) (BEX) was used to induce EAE in C57/BL6J mice. Mice were injecteds.c. with 200 g of MOG peptide in100 L of PBS emulsified in 100 L complete Freund's adjuvant (CFA) that was further supplemented with five mg mL?1 Mycobacterium tuberculosis (H37Ra). In addition, 500 ng pertussis toxin was injected i.p. on days zero and two. The RSK inhibitor (BI-D1870; 0.5 mg kg?1) was injected i.p. into mice two days after immunization with MOG peptide, and injection was repeated every other day for 11 days. Mice that received only dimethyl sulfoxide (DMSO) solution were used as controls. Paralysis was evaluated according to the following scale: zero, no disease; one, tail limpness; two, hind limb weakness; three, hind limb paralysis; four, forelimb weakness; five, quadriplegia; six, death. For histological analysis, CNS samples were fixed with 4% paraformaldehyde and sliced at 4 m, and then hematoxylin & eosin (H & E) staining was performed [4].
体外活性	方法：将HEK-293细胞与 BI-D1870（10 μM，15分钟，总共4小时）孵育为了检验BI-D1870是否能抑制细胞中的RSK活性，研究BI-D1870对HEK-293细胞中RSK催化其已知底物磷酸化的影响，使用PMA作为激动剂激活ERK1/ERK2和RSK亚型。结果：用 BI-D1870 孵育细胞可极大地抑制 PMA 诱导的 GSK3α 和 GSK3β 磷酸化，相比之下，BI-D1870在任何时间点对PMA诱导的ERK1/ERK2激活（由Raf和MKK1催化）或CREB在Ser位点的磷酸化几乎没有影响。[1] 方法：BI-D1870（1,2,3,4,5.28或者48小时）处理口腔癌细胞系 (SCC2095、SCC4、SCC9、Ca922 和 HSC-3) 和NHOK细胞，MTT检测这些细胞的生长情况。结果： BI-D1870 对 OSCC 细胞表现出剂量反应性抗增殖作用。[3] 方法：用 BI-D1870 （0.5,2μM）处理转染免疫荧光 GFP-LC3 的细胞 48 小时，并在共聚焦显微镜下观察；使用 DAPI 染色定位细胞核，用 BI-D1870 处理 48 小时的观察细胞中 LC3B 的蛋白质印迹。结果：BI-D1870 诱导自噬，LC3B-II 的蛋白质印迹表明这种诱导具有剂量依赖性。[3]
体内活性	方法：在用 MOG 肽免疫小鼠两天后，BI-D1870（0.5 mg/kg) 腹腔注射到小鼠体内，每隔一天重复注射一次，持续 11 天。结果：小鼠表现出延迟神经缺陷；BI-D1870 治疗对体重减轻有中等程度的保护作用。[4]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 6.88 mg/mL (17.56 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.2 mg/mL (18.39 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字	BI-D 1870 \| BI-D1870 \| inhibit \| Ribosomal S6 Kinase (RSK) \| S6K \| Inhibitor \| BI-D-1870 \| Autophagy \| BI D1870 \| BID1870
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相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗结直肠癌化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 谷氨酰胺代谢化合物库 \| 抗肝癌化合物库 \| 疼痛相关化合物库 \| 表型筛选靶点鉴定库

BI-D1870|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子