2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. PROTACs Aurora Kinase
  4. SK5527

SK5527 是一种选择性 AURKA PROTAC 降解剂，可降解 AURKA 蛋白，其对 AURKA 的 DC50 = 2 nM。SK5527 以 20 nM 的 IC50 值结合 NanoLuc-AURKA。SK5527 能有效降低 MYCN 扩增型神经母细胞瘤细胞中的 MYCN 水平，但其活性受 MDR1 介导的外排作用限制。SK5527 在体内能高效降低 AURKA 水平。SK5527 可用于神经母细胞瘤的相关研究。
(粉色: Aurora A 配体 (HY-179643)；蓝色: Cereblon E3 连接酶配体；黑色: 连接子)。

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SK5527

SK5527 Chemical Structure

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SK5527 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Aurora Kinase 亚型特异性产品:

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Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC50 = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC50 of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research[1]. (Pink: Aurora A ligand (HY-179643); Blue: Cereblon E3 ligase ligand; Black: linker).

IC50 & Target[1]

Aurora A

2 nM (DC50)

体外研究
(In Vitro)

SK5527 (0.01-10000 nM，1-48 h) 能在神经母细胞瘤和良性细胞系 (HEK293T，RPE) 中诱导降解 AURKA与 MYCN，在 MYCN 扩增细胞 (IMR-32，NGP，SJNB-8，SK-N-BE(2)-C的 DC50 分别为6，2，10 和 73 nM) 中表现出高效力，在其他细胞系 (SK-N-BE(2)-C，SK-N-AS，SJNB-1) 中活性降低并出现钩状效应，其诱导的 MYCN 耗竭是 AURKA 降解后发生的次级延迟事件，且需要同时结合 AURKA 和 CRBN 才能发挥降解作用 (IMR-32， NGP， SJNB-8， SK-N-BE(2)-C的 GI50 分别为 15，21，63，477 nM) ; 在非扩增细胞 (SK-N-SH， SK-N-AS 和 SJNB-1的 GI50 分别为 244，654，8635 nM) 及良性永生化细胞 RPE 和 HEK293T 细胞中 (GI50 为 460 和 408 nM) 中也是如此[1]。
SK5527 (10-10000 nM，72 h) 能有效抑制神经母细胞瘤细胞 (IMR-32，NGP，SJNB-8，SK-N-SH，SK-N-BE(2)-C，SJNB-1) 的生长[1]。
SK5527（100-1000 nM，处理 3 小时）的作用需要同时结合 AURKA 和 CRBN，能显著结合 AURKA 并具有优异的全激酶组选择性，可上调 PLK1、下调 HAND2 和 ESCO2，但不会下调 GSPT1、CSNK1A1、ZFP91、SALL4、ZNF654、ZNF787、E4F1 和 PATZ1[1]。
SK5527 在良性永生细胞系 HEK293T 和 RPE 中仅表现出适度的抑制效果，尽管它能强效降解 AURKA，DC50 值约为 0.5 μM[1]。
SK5527 (10-1000 nM，24-72 h) 的活性在 SK-N-SH，SK-N-BE(2)-C，SJNB-1，NGP，SJNB-8，IMR-32 等细胞中受 MDR1 介导的药物外排限制，但在 SK-N-AS 细胞中没有发现 (原因在于其 CRBN 低表达) [1]。

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

SK5527 相关抗体:

Western Blot Analysis[1]

Cell Line: IMR-32
Concentration: 500 nM
Incubation Time: 1, 4, 24 and 48 h
Result: Induced robust AURKA depletion already after 1 h, whereas MYCN co-depletion reached 50% only at 24h postexposure.

Cell Proliferation Assay[1]

Cell Line: IMR-32, NGP, SJNB 8 , SKN-SH, SK-N-BE(2)-C and SJNB-1
Concentration: 10, 100, 1000 and 10000 nM
Incubation Time: 72 h
Result: Had The strongest antiproliferative effects with GI50 values below 100 nM consistent with the observed potent AURKA degradation but less in SKN-SH, SK-N-BE(2)-C and SJNB-1.

Western Blot Analysis[1]

Cell Line: SK-N-BE(2)-C, SK-N-BE(2)-C, SK-N-SH, and SJNB-1
Concentration: 100 nM
Incubation Time: 24 h
Result: Exhibited high expression of multidrug resistance protein 1 (MDR1), encoded by the ABCB1 gene in SK-N-BE(2)-C, SK-N-SH, and SJNB-1.
Exhibited the highest MDR1 expression in our panel, cotreatment with 1 μM Tariquidar (HY-10550) significantly enhanced the AURKA degradation.

Cell Proliferation Assay[1]

Cell Line: NGP and SK-N-BE(2)-C cells
Concentration: 10, 100 and 1000 nM
Incubation Time: 48 h
Result: Dose-dependently increased of caspase 3/7 activity.

Cell Proliferation Assay[1]

Cell Line: NGP, SJNB-8, and SK-N-BE(2)-C
Concentration: 10, 100 and 1000 nM
Incubation Time: 72 h
Result: Exhibited growth-inhibitory activity comparable to AURKA inhibitor TAS-119, with nearly identical GI 50 values across cell lines.
体内研究
(In Vivo)

SK5527 (15 mg/kg，静脉注射或腹腔注射，单次给药) 可在 IMR-32 神经母细胞瘤细胞系来源的异种移植 (CDX) 小鼠模型中诱导 AURKA 蛋白耗竭[1]。

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

Animal Model: IMR-32 cells (1 × 10 7 cells in 0.2 mL volume) induced-female BALB/c nude mice[1]
Dosage: 15 mg/kg
Administration: i.v., or i.p. once
Result: Reduced AURKA protein levels in vivo at 4 and 8 h post-treatment after a single IV dose, followed by a return to baseline levels at 24 h but not observed in i.p. group
分子量

848.36

Formula

C42H49ClF3N11O3
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

SK5527 相关分类

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  • 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:

SK5527SK 5527SK-5527PROTACsAurora KinaseAURKA PROTAC degraderNanoLuc-AURKAMYCNneuroblasto2maInhibitorinhibitorinhibit

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目录号：
HY-179641
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