1. PROTAC Epigenetics Cell Cycle/DNA Damage
  2. PROTACs Aurora Kinase
  3. MS44

MS44 是一种强效的极光激酶 B (AURKB PROTAC) 降解剂 (DC50 = 103 nM)。MS44 能够以时间和泛素-蛋白酶体系统 (UPS) 依赖的方式有效降解 AURKB,并且对 AURKB 的选择性,而对 AURKA 和 AURKC 无选择性。MS44 能够有效抑制多种癌细胞系的增殖,并强效诱导 G2/M 阻滞。MS44 可用于研究 AURKB 依赖性肿瘤 (粉色:靶蛋白配体 (HY-175526);蓝色:E3 配体 (HY-112078);黑色:连接子;E3 配体 + 连接子 (HY-132938))。

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MS44

MS44 Chemical Structure

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  • 生物活性

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  • 参考文献

生物活性

MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors (Pink: Target protein ligand (HY-175526); Blue: E3 ligand (HY-112078); Black: Linker; E3 ligand + Linker (HY-132938))[1].

IC50 & Target[1]

Aurora B

103 nM (DC50)

VHL

 

体外研究
(In Vitro)

MS44 (Compound 18) (1 nM-10 μM, 1-96 h) 通过劫持 UPS,以浓度和时间依赖性方式有效降解 HPAF-11 细胞中的 AURKB,并在多种癌细胞系中也发挥了同样的作用[1]
MS44 (1 μM, 24-96 h) 抑制 HPAF-11、K562、U937、CFPAC-1、SW1783 和 HT-29 细胞的增殖[1]
MS44 (48 h) 诱导 U937 细胞 G2/M 期阻滞[1]

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

Cell Proliferation Assay[1]

Cell Line: HPAF-11 cells, K562 cells and U937 cells
Concentration: 1 μM
Incubation Time: 24, 48, 72 and 96 h
Result: Effectively suppressed the proliferation of HPAF-11 cells.

Western Blot Analysis[1]

Cell Line: HPAF-11, K562, U937, CFPAC-1, SW1783 and HT-29 cells
Concentration: 1, 3, 10, 30, 100, 300 nM, 1, 3, 10 μM for HPAF-11 and 1 μM for other cells
Incubation Time: 1, 2, 4, 8, 12, and 24 h for HPAF-11 and 24 h for other cells
Result: Induced significant degradation of AURKB in all cells.
Degraded AURKB in a concentration- and time-dependent manner in HPAF-11 cells by hijacking the UPS.
Selectively degraded AURKB over AURKA and AURKC in HPAF-11 cells.
分子量

1090.31

Formula

C57H72FN11O8S

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
  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

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产品名称:
MS44
目录号:
HY-175525
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