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D4476

D4476

产品编号 T2449   CAS 301836-43-1
别名: D 4476, Casein Kinase I Inhibitor

D4476 (Casein Kinase I Inhibitor) 是一种选择性和细胞渗透性的CK1抑制剂,在体外实验的IC50值为0.3 μM。

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D4476 Chemical Structure
D4476, CAS 301836-43-1
规格 价格/CNY 货期 数量
1 mg ¥ 253 现货
2 mg ¥ 359 现货
5 mg ¥ 587 现货
10 mg ¥ 855 现货
25 mg ¥ 1,470 现货
50 mg ¥ 2,360 现货
100 mg ¥ 3,480 现货
200 mg ¥ 4,980 现货
500 mg ¥ 7,580 现货
1 mL * 10 mM (in DMSO) ¥ 727 现货
产品目录号及名称: D4476 (T2449)
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选择批次  
纯度: 99.96%
纯度: 99.8%
纯度: 99.02%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).
靶点活性 CK1 (casein kinase 1):300 nM
体外活性 D4476 (10 μM) effectively inhibits CK1 and ALK5 with the activities of about 7% and 22% versus control group, respectively. In H4IIE hepatoma cells, D4476 specifically inhibits the phosphorylation of endogenous forkhead box transcription factor O1a (FOXO1a) on Ser322 and Ser325, without affecting the phosphorylation of other sites.[1] D4476 induces cytotoxicity in ANBL6, INA6 and RPMI8226 lines; MM1S and U266 lines are less sensitive; and OPM1 line is totally resistant. High concentrations (50 μM) D4476 induced toxicity in all multiple myeloma (MM) lines. In MM cells, D4476 increases the protein levels of TP53, P27, and FADD, as well as the cell cycle progression and induction of apoptosis.[2] Treatment of leukemia stem cells (LSCs) with D4476 shows highly selective killing of LSCs over normal HSPCs.[3]
激酶实验 CK1 kinase assay: All protein kinase assays (25 μL) are carried out at room temperature (21℃). Assays are performed for 40 min using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. The concentrations of magnesium acetate and [γ-33P]ATP (800 cpm/pmol) in the assays are 10 mM and 0.1 mM, respectively. Assays are initiated with MgATP and stopped by the addition of 5 μL of 0.5 M orthophosphoric acid. Aliquots are then spotted on to P30 ?ltermats, washed four times in 75 mM phosphoric acid to remove ATP, once in methanol, then dried and counted for radioactivity. CK1 δ (5-20 m-units), diluted in 20 mM Hepes, pH 7.5, 0.15 M NaCl, 0.1 mM EGTA, 0.1% (v/v) Triton X-100, 5 mM dithiothreitol, 50% (v/v) glycerol, is assayed against the peptide RRKDLHDDEEDEAMSITA in an incubation containing 20 mM Hepes, pH 7.5, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% (v/v) Triton X-100 and 0.5 mM substrate peptide.
细胞实验 MM cells are seeded in triplicate into 96-well plates in 100 μL culture media. D4476 is added to each well at concentrations of 0, 5, 10, 20, 30, 40, and 50 μM in another 100 μL culture media. Cell viability is measured with MTT at the 72 h drug exposure. Absorbance is measured at 570 nm with spectrophotometer.(Only for Reference)
别名 D 4476, Casein Kinase I Inhibitor
分子量 398.41
分子式 C23H18N4O3
CAS No. 301836-43-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 39.8 mg/mL (100 mM)

Ethanol: 19.9 mg/mL (50 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.51 mL 12.5499 mL 25.0998 mL 62.7494 mL
5 mM 0.502 mL 2.51 mL 5.02 mL 12.5499 mL
10 mM 0.251 mL 1.255 mL 2.51 mL 6.2749 mL
20 mM 0.1255 mL 0.6275 mL 1.255 mL 3.1375 mL
50 mM 0.0502 mL 0.251 mL 0.502 mL 1.255 mL
DMSO 100 mM 0.0251 mL 0.1255 mL 0.251 mL 0.6275 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
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Rena G, et al. EMBO Rep. 2004, 5(1), 60-65. 2. Hu Y, et al. Leukemia. 2015, 29(2), 474-482. 3. Järås M, et al. J Exp Med. 2014,211(4), 605-612. 4. Bain J, et al. Biochem J. 2003, 371(Pt 1), 199-204.
Emodin Silmitasertib sodium salt Ac-VDVAD-CHO PF-670462 NMS-P715 TBCA XL413 hydrochloride DMAT

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 Wnt/Hedgehog/Notch 通路化合物库 自噬库 细胞凋亡化合物库 表型筛选靶点鉴定库 抗代谢疾病化合物库 经典已知活性库 血管生成库 代谢化合物库 干细胞分化化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

D4476 301836-43-1 Angiogenesis Apoptosis Autophagy Metabolism Stem Cells Tyrosine Kinase/Adaptors ALK Casein Kinase inhibit D 4476 Inhibitor D-4476 Casein Kinase I Inhibitor inhibitor

 

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