LDN-192960
(Synonyms: 3-[(2,7-二甲氧基吖啶-9-基)硫基]丙胺) 目录号 : GC33086
An inhibitor of haspin and DYRK2
Cas No.:184582-62-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
LDN-192960 is an inhibitor of haspin protein kinase and dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 2 (DYRK2) with IC50 values of 10 and 48 nM, respectively.1 It is selective for haspin and DYRK2 over TRKB, CLK1, DYRK1A, DYRK3, ROS, HIPK1, HIPK2, PIM-1, and PIM-2 kinases (IC50s = 720-91,000 nM).
1.Cuny, G.D., Robin, M., Ulyanova, N.P., et al.Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitorsBioorg. Med. Chem. Lett.20(12)3491-3493(2010)
| Cas No. | 184582-62-5 | SDF | |
| 别名 | 3-[(2,7-二甲氧基吖啶-9-基)硫基]丙胺 | ||
| Canonical SMILES | NCCCSC1=C(C=C(OC)C=C2)C2=NC3=CC=C(OC)C=C31 | ||
| 分子式 | C18H20N2O2S | 分子量 | 328.43 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0448 mL | 15.2239 mL | 30.4479 mL |
| 5 mM | 0.609 mL | 3.0448 mL | 6.0896 mL |
| 10 mM | 0.3045 mL | 1.5224 mL | 3.0448 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Haspin participates in AURKB recruitment to centromeres and contributes to chromosome congression in male mouse meiosis
J Cell Sci 2022 Jul 1;135(13):jcs259546.PMID:35694956DOI:10.1242/jcs.259546
Chromosome segregation requires that centromeres properly attach to spindle microtubules. This essential step regulates the accuracy of cell division and must therefore be precisely regulated. One of the main centromeric regulatory signaling pathways is the haspin-H3T3ph-chromosomal passenger complex (CPC) cascade, which is responsible for the recruitment of the CPC to the centromeres. During mitosis, the haspin kinase phosphorylates histone H3 at threonine 3 (H3T3ph), an essential epigenetic mark that recruits the CPC, in which the catalytic component is Aurora B kinase (AURKB). However, the centromeric haspin-H3T3ph-CPC pathway remains largely uncharacterized in mammalian male meiosis. We have analyzed haspin functions by either its chemical inhibition with LDN-192960 in cultured spermatocytes, or the ablation of the Haspin gene in Haspin-/- mice. Our studies suggest that haspin kinase activity is required for proper chromosome congression both during meiotic divisions and for the recruitment of Aurora B and kinesin MCAK (also known as KIF2C) to meiotic centromeres. However, the absence of H3T3ph histone mark does not alter borealin (or CDCA8) and SGO2 centromeric localization. These results add new and relevant information regarding the regulation of the haspin-H3T3ph-CPC pathway and centromere function during meiosis.