化合物 BIX02189|T2416|TargetMol

BIX02189
1094614-85-3

￥341 1mg 起订

￥532 2mg 起订

￥747 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

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 BIX02189

英文名称：: BIX02189

CAS号：: 1094614-85-3

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：: 99.86%

产品类别：: 抑制剂

货号：: T2416

Product Introduction

Bioactivity

Name	BIX02189
Description	BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
Cell Research	The cells are serum starved for 20 hours prior to stimulation with sorbitol at a final concentration of 0.4 M for 20 minutes at 37 °C. BIX02189 is added 1.5 hours prior to the addition of sorbitol. The cells are harvested and lysed in 50 μL RIPA buffer containing Halt protease and phosphate inhibitors at 4 °C for 5-10 minutes. The lysates are centrifuged for 10 minutes at 14,000 rpm and 50 μL lysate is added to 50 μl 2× sample buffer and boiled for 4 minutes at 95 °C. Twenty microliters sample is run on SDS–PAGE 10% Tris-glycine gels and transferred to nitrocellulose. Western blotting is done with appropriate antibodies. (Only for Reference)
Kinase Assay	Catalytic assay: MEK5 protein isolated from the baculovirus expression system is used to measure kinase activity utilizing PKLight ATP Detection Reagent. The assay is performed using 15 nM GST-MEK5 and 0.75 μM ATP in assay buffer consisting of 25 mM Hepes, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4, 0.5 mM DTT and 1% DMSO in the presence of varying concentrations of BIX02189. The kinase reaction mixture is incubated for 90 minutes at room temperature followed by addition of 10 μL of ATP detection reagent for 15 minutes. The relative light unit (RLU) signal is measured and the RLU signals are converted to percent of control (POC) values for the determination of IC50 value.
In vivo	用BIX02189预处理以剂量依赖性方式抑制山梨醇诱导的HeLa细胞中ERK5的磷酸化,并且对ERK1/2,p38和JNK1/2 MAPKs的磷酸化没有抑制活性。在HeLa或HEK293细胞中仅用BIX02189处理24小时不显示任何细胞毒性作用。BIX02189抑制HeLa和HEK293细胞中MEK5/ERK5/MEF2C驱动的萤光素酶表达,IC50分别为 0.53 μM和0.26 μM。BIX02189抑制MEK5和ERK5催化活性,IC50分别为1.5 nM和59 nM。BIX02189抑制CSF1R(FMS),IC50为46 nM,但对相关激酶MEK1,MEK2,ERK1,p38α,JNK2,EGFR和STK16无活性,IC50 >3.7 μM。BIX02189增强山梨醇诱导的NRCM细胞凋亡,证实了ERK5在心肌细胞中的保护作用。BIX02189（10 μM）抑制ERK5磷酸化,并降低由异丙肾上腺素刺激的新生大鼠心肌细胞（NRCMs）中的肌细胞增强因子2（MEF2）转录活性。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 50 mg/mL (113.5 mM), Sonication is recommended. Ethanol : 74 mg/mL (168 mM)
Keywords	BIX02189 \| BIX-02189 \| BIX 02189
Inhibitors Related	Lidocaine hydrochloride \| Astragaloside IV \| Lidocaine \| Pirfenidone \| A 83-01 \| Honokiol \| Notoginsenoside R1 \| Tauroursodeoxycholate \| Galunisertib \| Alantolactone \| TBHQ \| Trametinib
Related Compound Libraries	Bioactive Compound Library \| Bioactive Compounds Library Max \| Cytokine Inhibitor Library \| Autophagy Compound Library \| MAPK Inhibitor Library \| Anti-Fibrosis Compound Library \| Apoptosis Compound Library \| Anti-Aging Compound Library \| NO PAINS Compound Library \| Tyrosine Kinase Inhibitor Library

BIX02189|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。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务