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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
AZ 3146, TTK 蛋白激酶抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
AZ3146是单极纺锤体1（Mps1）激酶抑制剂，IC50为35 nM，对FAK，JNK1，JNK2和Kit的抑制性较弱。A potent and selective monopolar spindle 1 (Mps1) kinase inhibitor
Information
AZ 3146 AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM, contributes to recruitment of CENP-E (kinesin-related motor protein), less potent to FAK, JNK1, JNK2, and Kit.
In vitro
AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~50% enter anaphase without aligning all of their chromosomes, and ~30% exit mitosis without undergoing obvious chromosome segregation. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequent recruitment of Mad1 and Mad2 to kinetochores is abolished. However, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1–C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core.
In vivo
Cell Data
cell lines：Ba/F3, Molm-13, Molm-14, HL60, AML193, KG-1, KG-1a, THP-1, and RS4;11
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
别名
亚利桑那州 3146
英文别名
9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AZ 3146
生化机理
AZ3146 是一种选择性 Mps1 抑制剂，IC50 约为 35 nM，有助于 CENP-E（驱动蛋白相关运动蛋白）的招募，对 FAK、JNK1、JNK2 和 Kit 的抑制作用较弱。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
TTK 蛋白激酶抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1CCC(CC1)OC2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(C(=O)N4C)C5CCCC5)OC
分子量
452.55
Reaxy-Rn
18988740
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18988740&ln=
技术文档
高级数据
关联靶点（人）
TTK
Tchem
双特异性蛋白激酶 TTK(Dual specificity protein kinase TTK)
(2 活性数据)
化学和物理性质
折光率
1.63
沸点
621.04 °C at 760 mmHg
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 F2414229 |
分析证书 | A408500 |
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