2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis Epigenetics
  3. MASTL Apoptosis Aurora Kinase PARP Caspase
  4. MKI-3

MKI-3 是一种选择性微管相关丝氨酸/苏氨酸激酶样 (MASTL) 抑制剂，IC50 为 5.72 nM，Kd 为 1.89 nM。MKI-3 可并破坏 MASTL-ENSA-Aurora A 信号轴。MKI-3 可诱导癌细胞出现染色体不稳定性、有丝分裂灾难和细胞凋亡 (apoptosis)。MKI-3 可用于三阴性乳腺癌的相关研究。

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MKI-3

MKI-3 Chemical Structure

CAS No. : 3084702-28-0

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MKI-3 相关抗体

Top Publications Citing Use of Products

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

查看 PARP 亚型特异性产品:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MKI-3 is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC50 of 5.72 nM and a Kd of 1.89 nM. MKI-3 disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 is applicable to research related to triple-negative breast cancer[1].

体外研究
(In Vitro)

MKI-3 可抑制细胞内 MASTL 活性，其 IC50 值为 114.9 nM[1]。
MKI-3 (72 h) 可抑制乳腺癌细胞系 4T1、MCF7、MDA-MB-231 和 BT549 的增殖，其 IC50 值分别为 42.01 nM、93.61 nM、91.44 nM 和 160.9 nM[1]。
MKI-3 (250 nM; 12 h) 可抑制 MASTL-ENSA-Aurora A 信号轴，在 BT549 和 4T1 乳腺癌细胞中诱导凋亡标志物[1]。
MKI-3 (250 nM; 24 h) 可激活 BT549 乳腺癌细胞中的 PP2A[1]。
MKI-3 (250 nM; 24 h) 可在 BT549 乳腺癌细胞中诱导有丝分裂缺陷，包括异常核形态、多极纺锤体和中心体异常[1]。
MKI-3 (250 nM; 48 h) 对 BT549 乳腺癌细胞的抗增殖活性部分由 PP2A 的激活介导，因为与 20 nM okadaic acid 共同处理可恢复细胞活力[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MKI-3 相关抗体:

Western Blot Analysis[1]

Cell Line: BT549 and 4T1 breast cancer cells
Concentration: 250 nM
Incubation Time: 12 h
Result: Reduced levels of phosphorylated ENSA (pENSA) and phosphorylated Aurora A (p-Aurora A), and increased levels of cleaved poly(ADP-ribose) polymerase (PARP) and gamma H2A histone family member X (γ-H2AX), markers of mitotic apoptosis.
体内研究
(In Vivo)

MKI-3 (8 mg/kg；腹腔注射；每日；2 周) 可显著抑制 4T1 三阴性乳腺癌小鼠模型中的肿瘤生长[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4T1 syngeneic mouse model[1]
Dosage: 8 mg/kg
Administration: i.p.; daily; 2 weeks
Result: Reduced mean nuclear size diameter.
Increased cells staining positive for phospho-histone H3 and cleaved caspase-3.
Significantly reduced phosphorylation of ENSA and Aurora A in tumor tissues, with near-complete suppression relative to controls.
分子量

385.42

Formula

C21H19N7O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MKI-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MKI-33084702-28-0MKI3MKI 3MASTLApoptosisAurora KinasePARPCaspaseMicrotubule‐associated serine/threonine kinase likepoly ADP ribose polymeraseendosulfine alphaBT549protein phosphatase 2AMCF74T1MDA-MB-231triple-negative breast cancerAurora AENSAInhibitorinhibitorinhibit

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