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LDN 209929 dihydrochloride Sale

目录号 : GC14901

haspin kinase inhibitor

LDN 209929 dihydrochloride Chemical Structure

Cas No.:1784281-97-5

规格 价格 库存 购买数量
10mg
¥2,340.00
现货
50mg
¥8,550.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

Target: haspin kinase

IC50: 55 nM

LDN 209929 dihydrochloride is a selective and potent haspin kinase inhibitor with IC50 value of 55 nM [1]. LDN 209929 dihydrochloride displays 180-fold selectivity on haspin kinase over DYRK2 [1].

Haspin, also known as Germ Cell-Specific Gene-2 (Gsg2), is a serine/threonine kinase expressed in several tissues (e.g., testis, thymus, bone narrow, and spleen), proliferating cells and neoplasms, including diffuse large B cell lymphomas and Burkitt’s lymphoma. Haspin’s kinase activity is required for completion of normal mitosis. Therefore, Haspin has emerged as a potential therapeutic target in oncology [1].

DYRKs (Dual-specificity Tyrosine-regulated Kinases), belong to the CMGC family of eukaryotic protein kinase, can be divided into class 1 kinases (DYRK1A and 1B) and class 2 kinases (DYRK2, 3, and 4), which are predominantly cytosolic. DYRKs participate in regulation of several signaling pathways, including Hedgehog signaling, caspase activity during apoptosis, cell cycle progression and mitosis, NFAT signaling in the brain and immune system, and p53 activation in response to DNA damage [1].

In vitro: N/A

In vivo: N/A

Reference:
1.  Cuny GD, Robin M, Ulyanova NP, Patnaik D, Pique V, Casano G, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010;20(12):3491-4.

Chemical Properties

Cas No. 1784281-97-5 SDF
化学名 3-((2-chloro-7-methoxyacridin-9-yl)thio)propan-1-amine
Canonical SMILES NCCCSC1=C2C(C=CC(OC)=C2)=NC3=CC=C(Cl)C=C31
分子式 C17H17ClN2OS.2HCl 分子量 405.77
溶解度 <40.58mg/ml in Water; <40.58mg/ml in DMSO 储存条件 Desiccate at RT
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4645 mL 12.3223 mL 24.6445 mL
5 mM 0.4929 mL 2.4645 mL 4.9289 mL
10 mM 0.2464 mL 1.2322 mL 2.4645 mL
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