化合物 Longdaysin|T5358|TargetMol

Longdaysin
1353867-91-0

￥177 1mg 起订

￥448 5mg 起订

￥713 10mg 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

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产品详情:

中文名称：: 化合物 Longdaysin

英文名称：: Longdaysin

CAS号：: 1353867-91-0

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：: 99.97%

产品类别：: 抑制剂

货号：: T5358

Product Introduction

Bioactivity

Name	Longdaysin
Description	Longdaysin is an inhibitor of CK1α and CK1δ (IC50s: 5.6/8.8 μM). It also can inhibit ERK2 (IC50: 52 μM).
Cell Research	2×10^5 cells were suspended in 100 μL serum-free medium containing the indicated concentrations of longdaysin, and then seeded in 24-transwell chambers with 8 μm pore membrane. The lower chamber contained medium with 20% FBS. After incubation at 37°C for 6 hours, the unmigrated cells on the upper side of membrane were removed by a cotton swab, and the migrated cells were stained with crystal violet and stained cells were photomicrographed. For invasion assays, the transwell chambers with 8 μm pore membranes were coated with Matrigel [2].
Kinase Assay	The CKIδ, CKIα, CDK7, and ERK2 kinase assays were performed on 384-well plates (10 μl volume). The reaction mixture was as follows: for CKIδ, 2 ng/μl CKIδ, 50 μM peptide substrate RKKKAEpSVASLTSQCSYSS corresponding to human PER2 Lys659-Ser674, and CKI buffer (40 mM Tris, 10 mM MgCl2, 0.5 mM DTT, 0.1 mg/ml BSA, pH 7.5); for CKIα, 1 ng/μl CKIα, 50 μM CKI peptide substrate, and CKI buffer; for CDK7, 5 ng/μl CDK7, 100 μM Cdk7/9 peptide substrate, and CKI buffer; for ERK2, 1.5 ng/μl ERK2, 0.8 μg/μl MBP, and ERK buffer (50 mM Tris, 10 mM MgCl2, 0.5 mM DTT, 1 mM EGTA, pH 7.5). Five hundred nl of compound was added to the mixture (final 5% DMSO), and the reaction was started by adding ATP (final 5 μM). After incubation at 30°C for 3h, 10 μl of Kinase-Glo Luminescent Kinase Assay reagent was added, and the luminescence was detected to determine the remaining ATP amount. All of the tested compounds did not inhibit luciferase activity directly [1].
Animal Research	MDA-MB-231 cells were injected s.c. into the right flank of nude mice (1×10^7 cells per mouse), and tumor growth was closely observed and measured every 3 days. When the tumors reached approximately 50 mm3, the mice were randomly divided into two groups (eight mice per group) and i.p. injected with the vehicle (0.8% DMSO/12% Cremophor/8% ethanol in normal saline) or 5 mg/kg longdaysin in vehicle every 3 days. This longdaysin dosage was selected based on results from preliminary experiments, and was well tolerated in the mouse model. Subsequently, tumor volumes were measured with a caliper and calculated as follows: 0.523×(length)×(width)2. After treatment for 3 weeks, the mice were sacrificed and the tumor tissues were collected and weighed before being fixed in buffered formalin [2].
In vitro	Longdaysin对CKIδ、CKIα、ERK2和CDK7的活性产生了抑制作用（IC50分别为8.8、5.6、52和29 μM），而对p38α的影响则较小。CKIδ缺陷细胞的周期比野生型细胞长1.1小时。在CKIδ缺陷细胞和野生型细胞中，Longdaysin以剂量依赖性方式延长了周期[1]。在乳腺癌Hs578T和MDA-MB-231细胞中，micromolar浓度的Longdaysin减弱了LRP6和DVL2的磷酸化，并降低了活性β-catenin和总β-catenin的表达，从而导致Wnt靶基因Axin2、DKK1、LEF1和Survivin的下调[2]。
In vivo	在MDA-MB-231乳腺癌异种移植模型中，longdaysin与Wnt/β-catenin信号传导的抑制相关，抑制了肿瘤生长[2]。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 100 mg/mL (298.21 mM) H2O : Insoluble
Keywords	ERK \| Cyclin dependent kinase \| inhibit \| CDK \| Inhibitor \| Longdaysin \| Casein Kinase \| Extracellular signal regulated kinases
Inhibitors Related	Lidocaine hydrochloride \| Astragaloside IV \| Lidocaine \| Sodium Oxamate \| Honokiol \| Ribociclib \| CASIN \| Tauroursodeoxycholate \| Palbociclib \| Dinaciclib \| TBHQ \| Abemaciclib
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Bioactive Compounds Library Max \| Cell Cycle Compound Library \| Anti-Colorectal Cancer Compound Library \| Kinase Inhibitor Library \| Anti-Aging Compound Library \| HIF-1 Signaling Pathway Compound Library \| Pain-Related Compound Library

Longdaysin|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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