2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. PROTACs Aurora Kinase
  4. SK4454

SK4454 是一种选择性 AURKA PROTAC 降解剂，可降解AURKA蛋白对 AURKA 的IC50 = 8 nM。SK4454 以 20 nM的IC50 值结合 NanoLuc-AURKA。SK4454 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。SK4454 在体内能高效降低 AURKA 水平。SK4454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 配体 (HY-179642)；黑色: 连接子 (HY-69260))。

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SK4454

SK4454 Chemical Structure

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Customer Review

SK4454 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SK4454 is a selective AURKA PROTAC degrader degrading AURKA with IC50 = 8 nM. MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK4454 efficiently reduced AURKA levels in vivo. SK4454 can be used for neuroblastoma research[1]. (Pink: Aurora A ligand (HY-179643); Blue: Cereblon ligand (HY-179642); Black: linker (HY-69260)).

IC50 & Target[1]

Aurora A

20 nM (IC50)

Aurora A

1 nM (Ki)

Aurora B

7644 nM (Ki)

Cereblon

4060 nM ()

体外研究
(In Vitro)

SK4454 (0.01-10000 nM，1-48 小时) 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 6，8，23 和 270 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 8， 14，53，1111 nM) ; 在非扩增细胞 (SK-N-SH， SK-N-AS 和 SJNB-1 的 GI50 分别为 430，994，13437 nM) 及良性永生化细胞 RPE (GI50 为 221 nM) 中也是如此[1]。
SK4454 (10-10000 nM，72 小时) 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]。
SK4454 (10-1000 nM，24-72 小时) 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.

SK4454 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: Has 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: Exhibit 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.
Exhibits the highest MDR1 expression in our panel, cotreatment with 1 μM Tariquidar (HY-10550) significantly enhanced the AURKA degradation.

Apoptosis Analysis[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)

SK4454 (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

830.37

Formula

C42H50ClF2N11O3
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

SK4454 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

SK4454SK 4454SK-4454PROTACsAurora KinaseAURKANanoLuc-AURKAMYCNMDR1-mediated effluxneuroblastomaInhibitorinhibitorinhibit

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