2. PROTAC Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. PROTACs Apoptosis Caspase Aurora Kinase
  4. SK2188

SK2188 是一种高效且有选择性的靶向 AURKA 的 PROTAC 降解剂 (DC50 = 3.9 nM)。SK2188 诱导 DNA 损伤与细胞凋亡 (Apoptosis)。SK2188 间接降解 MYCN，抑制肿瘤细胞增殖，对 MYCN 扩增型神经母细胞瘤的研究提供思路 (粉色: AURKA ligand: MK-5108 (HY-13252); 蓝色: Thalidomide (HY-14658); 黑色: Linker: Amino-PEG4-alcohol (HY-W008005))。

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SK2188 Chemical Structure

SK2188 Chemical Structure

CAS No. : 3038446-94-2

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SK2188 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 Caspase 亚型特异性产品:

查看所有亚型
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

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

SK2188 is a highly efficient and selective PROTAC degrader targeting AURKA (DC50 = 3.9 nM). SK2188 induces DNA damage and cell apoptosis. SK2188 indirectly degrades MYCN, inhibits tumor cell proliferation, and provides insights into the study of MYCN-amplified neuroblastoma (Pink: AURKA ligand: MK-5108 (HY-13252); Blue: Thalidomide (HY-14658); Black: Linker: Amino-PEG4-alcohol (HY-W008005))[1].

IC50 & Target[1]

Caspase 3

 

Caspase-7

 

Aurora A

 

Cereblon

 

体外研究
(In Vitro)

SK2188 (10-10000 nM, 48-120 h) 在 MYCN 扩增细胞中高效抑制增殖，且对来源于患者的类器官细胞有效[1]。

SK2188 (10-1000 nM, 24 h) 在 NGP 细胞中通过诱导凋亡来抑制细胞生长[1]。

SK2188 (10-1000 nM, 1-72 h) 在 NGP 细胞中使 AURKA 降解引发 DNA 损伤和复制应激[1]。

SK2188 (100-1000 nM, 3h) 在 NGP 细胞中具有高靶点选择性和降解特异性[1]。

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

SK2188 相关抗体:

Cell Viability Assay[1]

Cell Line: NGP cells, IMR-32 cells, N206 cells, SK-N-AS cells, NB patient-derived organoids cells
Concentration: 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time: 48 h (NGP cells, IMR-32 cells, N206 cells, SK-N-AS cells); 120 h (NB patient-derived organoids cells)
Result: Inhibited cell viability with IC50s of 31.9 nM and 21.5 nM in NGP and IMR-32 cells, respectively, which were significantly lower than those of the parent inhibitor MK-5108 (IC50s: 348.9 nM and 199.3 nM).
Inhibited cell viability with IC50s of 131.3 nM and 26.4 nM in MYCN-amplified organoids NB139 and NB067, respectively, which were significantly lower than those of the parent inhibitor MK-5108 (IC50s: 899.7 nM and 75.3 nM).

Apoptosis Analysis[1]

Cell Line: NGP cells
Concentration: 10 nM, 100 nM, 1000 nM
Incubation Time: 24 h
Result: Significantly activated Caspase 3/7 at 10 nM and exerted a stronger apoptosis-inducing effect than MK-5108 at 1000 nM.

Western Blot Analysis[1]

Cell Line: NGP neuroblastoma cells
Concentration: 10 nM, 100 nM, 500 nM, 1000 nM
Incubation Time: 1 h, 3 h, 6 h, 24 h, 48 h, 72 h
Result: Induced 89 % AURKA degradation (DC50 = 3.9 nM) at 24 hours. Reduced MYCN protein levels (73 % degradation at 72 hours). Increased DNA damage markers (γH2AX, pCHK1)at 24 hours.
分子量

893.38

Formula

C43H46ClFN6O10S
CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

SK2188 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:

SK21883038446-94-2JB325SK 2188SK-2188JB 325JB-325PROTACsApoptosisCaspaseAurora KinaseNGP cellsAURKANeuroblastomaMYCNInhibitorinhibitorinhibit

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