2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. NSC-134754

NSC-134754 是脱氢依米丁衍生物，同时也是热休克蛋白诱导抑制剂。NSC-134754 在转录后水平发挥作用，靶向 Hsp72 和 Hsp27，且不会改变整体蛋白质合成、HSF-1 的转录活性或 Hsp mRNA 水平。NSC-134754 在临床前模型中无显著毒性，可使癌细胞对蛋白酶体抑制剂和 Hsp90 抑制剂增敏。NSC-134754 可用于多发性骨髓瘤、前列腺癌、结肠癌的相关研究。

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NSC-134754

NSC-134754 Chemical Structure

CAS No. : 75041-32-6

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NSC-134754 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NSC-134754 is a dehydroemetine derivative and heat shock protein induction inhibitor. NSC-134754 acts at the post-transcriptional level, targets Hsp72 and Hsp27, and does not alter general protein synthesis, HSF-1 transcriptional activity, or Hsp mRNA levels. NSC-134754 shows no significant toxicity in preclinical models and sensitizes cancer cells to proteasome and Hsp90 inhibitors. NSC-134754 can be used for the research of multiple myeloma, prostate carcinoma, colon carcinoma[1].

体外研究
(In Vitro)

NSC-134754 可抑制 CHO 细胞中热休克诱导的 Hsp72 表达，其 IC50 为 1 μM，且细胞毒性 IC50 为 5 μM[1]。
NSC-134754 (热休克前 16 h，给药浓度 1-2 μM) 可在 1 μM 浓度下强效抑制 CHO 细胞中热休克诱导的 Hsp72 表达，在 2 μM 浓度下则可完全抑制该诱导作用[1]。
NSC-134754 (1-2 μM; 24 h) 不会抑制 CHO 细胞中的总蛋白质合成[1]。
NSC-134754 (2 μM；预孵育 5 小时，在热休克及过夜恢复阶段持续存在) 可部分抑制热休克处理的 PC-3 细胞中 HSF-1 依赖的转录 (抑制率 40%)[1]。
NSC-134754 (提前孵育 5 小时，热休克全程存在) 在 PC-3 细胞中不会抑制热休克诱导的 Hsp72 mRNA 转录[1]。
NSC-134754 (热休克及恢复阶段给药) 可强效抑制多株细胞系中热休克诱导的 Hsp72 表达，其中 MM.1S 细胞与 MEF 细胞中的抑制率达 100%，CHO 细胞中为 99%，PC-3 细胞中为 85%[1]。
NSC-134754 (2 μM; 5 h pre-incubation, present during overnight Velcade treatment) 可完全抑制蛋白酶体抑制剂 (Velcade) 诱导的 MM.1S 细胞中 Hsp72 的表达上调[1]。
NSC-134754 (预孵育 5 h，在整夜 radicicol 处理全程存在，浓度 2 μM) 可在 MM.1S 细胞中使 Hsp90 抑制剂 (radicicol) 诱导的 Hsp72 表达被抑制 90%[1]。
NSC-134754 (2 μM；在蛋白酶体抑制剂处理期间) 可在 PC-3 细胞中抑制由蛋白酶体抑制剂 (MG132) 诱导的 Hsp72 表达，抑制率达 90%[1]。
NSC-134754 (在 Hsp90 抑制剂处理过程中给予 2 μM) 可在 PC-3 细胞中抑制由 Hsp90 抑制剂 (17-AAG) 诱导的 Hsp72 表达，抑制率达 70%[1]。
NSC-134754 (2 μM; 5 h pre-incubation, present during 48 h radicicol treatment) 可使 MM.1S 多发性骨髓瘤细胞对 Hsp90 抑制剂 (根赤壳菌素 HY-N6769) 诱导的细胞凋亡增敏，该效应通过 PARP 切割水平升高得到验证[1]。

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

NSC-134754 相关抗体:

Western Blot Analysis[1]

Cell Line: CHO cells
Concentration: 1 μM; 2 μM
Incubation Time: 16 h (prior to heat shock)
Result: Strongly inhibited heat shock-induced Hsp72 induction at 1 μM.
Completely inhibited heat shock-induced Hsp72 induction at 2 μM.

Western Blot Analysis[1]

Cell Line: CHO cells, MM.1S cells, PC-3 cells, MEF cells
Concentration: 2 μM
Incubation Time: during heat shock and recovery
Result: Inhibited heat shock-induced Hsp72 induction by 99% in CHO cells.
Inhibited heat shock-induced Hsp72 induction by 100% in MM.1S cells.
Inhibited heat shock-induced Hsp72 induction by 85% in PC-3 cells.
Inhibited heat shock-induced Hsp72 induction by 100% in MEF cells.

Western Blot Analysis[1]

Cell Line: MM.1S cells
Concentration: 2 μM
Incubation Time: 5 h (pre-incubation; present during overnight Velcade treatment)
Result: Completely inhibited Velcade-induced Hsp72 induction in MM.1S cells.

Western Blot Analysis[1]

Cell Line: MM.1S cells
Concentration: 2 μM
Incubation Time: 5 h (pre-incubation; present during overnight radicicol treatment)
Result: Inhibited radicicol-induced Hsp72 induction by 90% in MM.1S cells.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 2 μM
Incubation Time: during proteasome inhibitor treatment
Result: Inhibited MG132-induced Hsp72 induction by 90% in PC-3 cells.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 2 μM
Incubation Time: during Hsp90 inhibitor treatment
Result: Inhibited 17-AAG-induced Hsp72 induction by 70% in PC-3 cells.

Western Blot Analysis[1]

Cell Line: MM.1S cells
Concentration: 2 μM
Incubation Time: 5 h (pre-incubation; present during 48 h radicicol treatment)
Result: Significantly increased radicicol-induced PARP cleavage in MM.1S cells.
分子量

418.57

Formula

C27H34N2O2
CAS 号
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

NSC-134754 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:

NSC-13475475041-32-6NZ-28NSC134754NSC 134754NZ28NZ 28HSPHeat shock proteinsHsp27Hsp72HSF-1colon carcinomaMEF cellsCHO cellsMM.1S cellsPC-3 cellsprostate carcinomamultiple myelomaInhibitorinhibitorinhibit

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