2. Protein Tyrosine Kinase/RTK Apoptosis JAK/STAT Signaling Stem Cell/Wnt PROTAC
  3. Anaplastic lymphoma kinase (ALK) Apoptosis STAT PROTACs
  4. ALK degrader 1

ALK degrader 1 是一种强效的基于疏水标签技术 (HyT) 的降解剂，它依赖泛素-蛋白酶体系统降解 EML4-ALK (DC50 = 0.13 μM)。ALK degrader 1 在 ALK 依赖性细胞系中表现出优越的 ALK 降解活性与抗增殖作用，但对 ALK 融合阴性细胞则无明显细胞毒性。ALK degrader 1 能诱导细胞发生 G0/G1 期周期阻滞并促进细胞凋亡 (apoptosis)。其不仅可以高效降解 ALK 蛋白，还能阻断 STAT3 等关键下游信号轴。ALK degrader 1 在体内高效诱导 EML4-ALK 降解。ALK degrader 1 适用于 ALK 相关疾病的研究。

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ALK degrader 1

ALK degrader 1 Chemical Structure

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ALK degrader 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research[1].

体外研究
(In Vitro)

ALK degrader 1 (compound H7) (72 小时) 在 ALK 依赖性细胞系中表现出抗增殖作用，在 H3122 细胞中的 IC50 为 0.23 μM，在 Karpas 299 细胞中的 IC50 为 0.19 μM[1]。
ALK degrader 1 (0.5-5 μM，24 小时) 可有效降解 H3122 细胞中的 EML4-ALK，在0.5 μM 下即可实现超过80 %的降解；而在 Karpas 299 细胞中对 NPM-ALK 的降解活性相对较弱，在 5 μM 下降解率约为70 %[1]。
ALK degrader 1 (0.1-5 μM，2–24 小时) 是一种强效的 EML4-ALK 降解剂 (DC50 = 0.13 μM)，具有快速、持续的降解特性，可有效抑制 H3122 细胞中的 ALK 磷酸化和下游 STAT3 信号通路[1]。
ALK degrader 1 (2 μM，24 小时) 在撤药后，仍能维持 EML4-ALK 的降解效果达 48 小时[1]。
ALK degrader 1 (0.5-2 μM，24 小时) 可有效抑制 H3122 细胞中的有丝分裂进程，引发 G0/G1 期停滞，从而诱导细胞凋亡[1]。
ALK degrader 1 (2 μM，24 小时) 上调 ALK mRNA 表达，同时促进 ALK 与 Hsp70 的结合，其降解作用可被 MG-132 (HY-13259) 显著抑制，表明该降解过程依赖于泛素-蛋白酶体系统[1]。
ALK degrader 1 (0.1-1 μM，72 小时) 对 ALK 阴性肿瘤细胞 (A549) 和正常肺上皮成纤维细胞 (HFL-1) 表现出良好的选择性，且无明显毒副作用，表明其安全性良好[1]。

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

ALK degrader 1 相关抗体:

Western Blot Analysis< sup>[1]

Cell Line: H3122 and Karpas 299 cells
Concentration: 0.5, 1, 5 μM
Incubation Time: 24 h
Result: Effectively degraded EML4-ALK in H3122 cells at 5 μM after 24 h.
Exhibited substantial EML4-ALK degradation efficacy even at 0.5 μM, with more than 80 % reduction observed in Karpas 299 cells.
Showed reduced degradation activity against NPM-ALK in Karpas 299 cells compared to its activity against EML4-ALK in H3122 cells.
Demonstrated appreciable NPM-ALK degradation in Karpas 299 cells, achieving approximately 70 % degradation at 5 μM.

Western Blot Analysis< sup>[1]

Cell Line: H3122 cells
Concentration: 0.1, 0.5, 1, 2, 5 μM
Incubation Time: 2, 4, 8, 16, 24 h
Result: Exhibited a concentration-dependent ability to degrade EML4-ALK in H3122 cells, with complete degradation observed and a DC50 of 0.13 μM.
Significant reduced ALK levels in H3122 cells at 0.5, 1 and 2 μM for 24 h.
Decreased ALK phosphorylation in H3122 cells at 0.1 μM.
Decreased p-STAT3 levels but did not change STAT3 levels in H3122 cells.
(2 μM)Induced effective and sustained degradation of EML4-ALK in H3122 cells, reaching approximately 30 % at 2 h, peaking by 4 h, maintaining suppression to 23 % at 24 h.

Western Blot Analysis< sup>[1]

Cell Line: H3122 cells
Concentration: 2 μM
Incubation Time: 24 h
Result: Maintained low EML4-ALK levels for 48 hours after removal.

Cell Cycle Analysis< sup>[1]

Cell Line: H3122 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Significantly increased the G0/G1 phase cell population and reduced the G2 phase population compared to control after 24 h at 2 μM.
Significantly increased the sub-G0 phase cell population.

Apoptosis Analysis< sup>[1]

Cell Line: H3122 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Increased the proportion of apoptotic cells from 9.41 % to 21.07 % after 24 h at 2 μM.

Cell Proliferation Assay< sup>[1]

Cell Line: H3122, HFL-1 and A549 cells.
Concentration: 0.1, 0.5, 1 μM
Incubation Time: 72 h
Result: Inhibited H3122 cell proliferation by 30 % at 0.1 μM, while the inhibition rates for A549 and HFL-1 cells were 14 % and 12 %, respectively.
Iinhibited the proliferation of over 80 % of H3122 cells at 0.5 μM, but showed minimal activity against HFL-1 and A549 cells.
Exhibited a 90 % inhibition rate against H3122 cells at 1 μM, while its toxicity toward HFL-1 and A549 cells remained very low.
体内研究
(In Vivo)

ALK degrader 1 (20 mg/kg，静脉注射，单次给药) 可有效降解 H3122 异种移植小鼠模型中肿瘤组织中的 EML4-ALK 蛋白[1]。

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

Animal Model: Female BALB/c nude mice (4 weeks old) subcutaneously inoculated with H3122 cells[1]
Dosage: 20 mg/kg
Administration: i.v., once
Result: Exhibited sustained EML4-ALK degradation, detectable by 12 hours post-treatment and achieving over 85% by 36 hours.
分子量

617.82

Formula

C39H47N5O2
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

ALK degrader 1 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:

ALK degrader 1ALK degrader1ALK degrader-1Anaplastic lymphoma kinase (ALK)ApoptosisSTATPROTACsAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALK degraderdegradation activityantiproliferativeALK-dependent cell linesH3122 cellsKarpas 299 cellscell cycle arrestapoptosisSTAT3EML4-ALKxenograft mouse modelALK-related diseasesInhibitorinhibitorinhibit

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