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(Z)-SMI-4a

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产品编号 T3058Cas号 438190-29-5
别名 TCS PIM-1 4a, SMI-4a

(Z)-SMI-4a (TCS PIM-1 4a) 是一种选择性的,细胞可渗透的且具有 ATP 竞争性的 Pim-1抑制剂,IC50为 24 μM,Ki 为 0.6 μM。它还抑制 Pim-2,IC50为 100 μM,具有抗癌活性。

(Z)-SMI-4a

(Z)-SMI-4a

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纯度: 99.44%
产品编号 T3058 别名 TCS PIM-1 4a, SMI-4aCas号 438190-29-5

(Z)-SMI-4a (TCS PIM-1 4a) 是一种选择性的,细胞可渗透的且具有 ATP 竞争性的 Pim-1抑制剂,IC50为 24 μM,Ki 为 0.6 μM。它还抑制 Pim-2,IC50为 100 μM,具有抗癌活性。

规格价格库存数量
5 mg¥ 495现货
10 mg¥ 786现货
50 mg¥ 2,280现货
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产品介绍

生物活性
产品描述
(Z)-SMI-4a (TCS PIM-1 4a) is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM.
靶点活性
Pim1:21 nM
体外活性
口服SMI-4a后1小时,与对照组小鼠肿瘤相比,p70 S6K磷酸化减少,而总的p70 S6K表达不变.每天60 mg/kg SMI-4a处理两次,明显降低肿瘤尺寸,且具有良好的耐受性.
体内活性
5 μM SMI-4a抑制胰腺癌和白血病细胞生长。SMI-4a降低前列腺和造血细胞中Pim靶点的磷酸化。SMI-4a引起细胞周期停滞并逆转Pim-1的抗凋亡活性。SMI-4a是Pim1的ATP竞争性抑制剂,IC50为17 nM。SMI-4a显示Pim1对一组激酶具有高选择性。SMI-4a抑制已知底物即翻译阻遏物4E-BP1的Pim-1的体外磷酸化。SMI-4a增加细胞核中p27Kip1的量。SMI-4a处理诱导MAPK通路上调。SMI-4a处理pre-T-LBL,抑制mTOR通路。
激酶实验
Scintillation Proximity Assay: Methyltransferase activity assays are performed by monitoring the incorporation of tritiumlabeled methyl group from S-adenosylmethionine (3H-SAM) to biotinylated peptide substrates using Scintillation Proximity Assay (SPA) for PRC2-EZH2 trimeric complex (EZH2:EED:SUZ12), PRC2-EZH1 pentameric complex (EZH1:EED:SUZ12:RBBP4:AEBP2), SETD7, G9a, GLP, SETDB1, SETD8, SUV420H1, SUV420H2, SUV39H2, MLL1 tetrameric complex (MLL:WDR5:RbBP5:ASH2L), PRMT1, PRMT3, PRMT5-MEP50 complex and SMYD2. The reaction buffer for SMYD2 and SMYD3 is 50 mM Tris pH 9.0, 5 mM DTT, 0.01% TritonX-100; for G9a, GLP and SUV39H2 is 25 mM potassium phosphate pH 8.0, 1 mM EDTA, 2 mM MgCl2 and 0.01% Triton X-100; and for other HMTs 20 mM Tris pH 8.0, 5 mM DTT, 0.01% TritonX-100. To stop the enzymatic reactions, 10 μL of 7.5 M guanidine hydrochloride is added, followed by 180 μL of buffer, mixed and transferred to a 384-well FlashPlate. After mixing, the reaction mixtures are incubated and the CPM counts are measured using Topcount plate reader. The CPM counts in the absence of compound for each data set are defined as 100% activity. In the absence of the enzyme, the CPM counts in each data set are defined as background (0%). IC50 values are determined using compound concentrations ranging from 100 nM to 100 μM. The IC50 values are determined using SigmaPlot software. EZH2-Y641F assays are performed using 30 nM of enzyme in 20 mM Tris pH 8, 5 mM DTT, 0.01% Triton X-100, 5 μM SAM and 1 μM of H3 (1-24) peptide (same as for the wild-type PRC2-EZH2 complex). For DNMT1, the assay is performed using hemimethylated dsDNA as a substrate. The dsDNA substrate is prepared by annealing two complementary strands (biotintlated forward strand: BGAGCCCGTAAGCCCGTTCAGGTCG and reverse strand: CGACCTGAACGGGCTTACGGGCTC), synthesized by Eurofins MWG Operon. Reaction buffer is 20 mM Tris-HCl, pH 8.0, 5 mM DTT, 0.01% Triton X-100.Methyltransferase activity assays for DOT1L is performed using Filter-plates. Reaction mixtures in 20 mM Tris-HCl, pH 8.0, 5 mM DTT, 2 mM MgCl2 and 0.01% Triton X-100 are incubated at room temperature for 1h, 100 μL 10% TCA is added, mixed and transferred to filter-plate. Plates are centrifuged at 2000 rpm for 2 min followed by 2 additional 10% TCA wash and one ethanol wash (180 μL) followed by centrifugation. Plates are dried and 100 μL MicroO is added and centrifuged. 70 μL MicroO is added and CPM are measured using Topcount plate reader.
别名TCS PIM-1 4a, SMI-4a
化学信息
分子量273.23
分子式C11H6F3NO2S
CAS No.438190-29-5
SmilesFC(F)(F)C1=CC=CC(\C=C2\SC(=O)NC2=O)=C1
密度1.530 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 27.3 mg/mL (100 mM)
DMSO: 65 mg/mL (237.89 mM), Sonication is recommended.
溶液配制表
1mg5mg10mg50mg
1 mM3.6599 mL18.2996 mL36.5992 mL182.9960 mL
5 mM0.7320 mL3.6599 mL7.3198 mL36.5992 mL
10 mM0.3660 mL1.8300 mL3.6599 mL18.2996 mL
20 mM0.1830 mL0.9150 mL1.8300 mL9.1498 mL
50 mM0.0732 mL0.3660 mL0.7320 mL3.6599 mL
100 mM0.0366 mL0.1830 mL0.3660 mL1.8300 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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