化合物 TG003|T1901|TargetMol

(E/Z)-TG003
300801-52-9

￥253 1mg 起订

￥356 2mg 起订

￥668 5mg 起订

上海更新日期：2024-09-29

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 TG003

英文名称：: (E/Z)-TG003

CAS号：: 300801-52-9

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：: 99.04%

产品类别：: 抑制剂

货号：: T1901

Product Introduction

Bioactivity

名称	(E/Z)-TG003
描述	(E/Z)-TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor.
细胞实验	2 × 105 HeLa cells or 1.5 × 105 COS-7 cells resuspended in 2 mL of medium are plated on 6-well dishes, and 2 μL of 10 mM TG003 dissolved in Me2SO (final concentration at 10 μM), or 2 μL of Me2SO, is added to some wells. Cells are trypsinized, and the density is counted every 24 h for 3 days. Cells are then fixed with 1 mL of ice-cold 70% ethanol, washed with PBS, incubated in 1 ml of PBS containing 1 μg/mL DNase-free RNase A and 50 μg/mL propidium iodide for 20 min at 37 °C, and proceeded to cell cycle analysis by FACSCalibur.(Only for Reference)
激酶实验	In Vitro Kinase Assay : Kinase activity of Clks and SRPKs is assayed in a reaction mixture, containing 200 mM Tris-HCl (pH 7.5), 12.5 mM MgCl2, 8 mM dithiothreitol, 4 mM EGTA, 1–20 μM ATP, 1 μCi of [γ-32P]ATP, 1 μg of synthetic peptide of SF2/ASF RS domain (NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH), and 0.1–1 μg of purified kinases in a final volume of 40 μL. cAMP-dependent protein kinase activity is assayed in a reaction mixture containing 80 mM Tris-HCl (pH 7.5), 12.5 mM MgCl2, 8 mM dithiothreitol, 4 mM EGTA, 10 μM ATP, 1 μCi of [γ-32P]ATP, 5 μg of histone H1, and 1 μg of catalytic subunit of rat cAMP-dependent protein kinase purified. Protein kinase C activity is assayed in a reaction mixture containing 200 mM Tris-HCl (pH 7.5), 12.5 mM MgCl2, 1 mM CaCl2, 80 μg/mL phosphatidylserine, 8 μg/mL diolein, 10 μM ATP, 1 μCi of [γ-32P]ATP, 5 μg of histone H1, and 2 μL of partially purified rat protein kinase C. The final concentration of Me2SO is adjusted to 1% regardless of inhibitor concentration. The reaction mixture is incubated at 30 or 25 °C for mammalian or Xenopus recombinant proteins, respectively, for 10 min, and a half-portion is spotted on P81 phosphocellulose membrane. The kinase assay conditions, including the incubation period and concentration of kinases and substrates, are optimized to maintain the linearity during incubation. The membrane is washed with 5% phosphoric acid solution (SF2/ASF RS domain) or 5% trichloroacetic solution (histone H1) at least over 15 min. The radioactivity is measured using a liquid scintillation counter. The net radioactivity is deduced by subtracting the background count from the reaction mixture without kinase, and the data are expressed as the percentage to the control sample containing the solvent.
体外活性	10 μM TG003能够治疗非洲爪蟾体内过度Clk活性诱导的胚胎缺陷.
体内活性	TG003通过抑制IL-1β异核RNA的剪接阻断血小板产生IL-1β RNA。在3T3-L1脂肪细胞分化过程中,TG003也阻断PKCβII的可变剪接和PPARγ1和PPARγ2的表达。TG003通过抑制Clk1/Sty介导的磷酸化抑制人类β珠蛋白在体外的SF2/ASF依赖性剪接。TG003抑制哺乳动物细胞中Clk1/Sty激酶活性,而对10 μM浓度的HeLa和COS-7细胞的生长没有毒性作用。
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 : 6 mg/mL (24.06 mM), Heating is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	(E/Z) TG003 \| Cyclin dependent kinase \| (E/Z)-TG-003 \| site \| tumor \| Wilm's \| TG-003 \| splice \| inhibit \| mutation \| Inhibitor \| TG 003 \| CDK \| (E/Z)-TG003 \| cancer \| (E/Z)TG003 \| (E/Z)-TG 003 \| breast
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相关库	抑制剂库 \| 抗乳腺癌化合物库 \| 经典已知活性库 \| 抗癌化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 细胞凋亡化合物库 \| 抗衰老化合物库 \| NO PAINS 化合物库 \| PPI抑制剂库

TG003|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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