NSC-134754
CAS No. : 75041-32-6
(Synonyms: NZ-28)
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| Cat. No. : | HY-123303 |
| M.Wt: | 418.57 |
| Formula: | C27H34N2O2 |
| Purity: | >98 % |
| Solubility: |
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].
In Vitro:NSC-134754 inhibits heat shock-induced Hsp72 induction in CHO cells with an IC50 of 1 μM and has a cellular toxicity IC50 of 5 μM[1].
NSC-134754 (1-2 μM; 16 h prior to heat shock) potently inhibits heat shock-induced Hsp72 induction in CHO cells at concentrations of 1 μM and completely inhibits this induction at 2 μM[1].
NSC-134754 (1-2 μM; 24 h) does not inhibit general protein synthesis in CHO cells[1].
NSC-134754 (2 μM; 5 h pre-incubation, present during heat shock and overnight recovery) partially inhibits HSF-1-dependent transcription (40% reduction) in heat-shocked PC-3 cells[1].
NSC-134754 (2 μM; 5 h pre-incubation, present during heat shock) does not inhibit heat shock-induced Hsp72 mRNA transcription in PC-3 cells[1].
NSC-134754 (2 μM; during heat shock and recovery) potently inhibits heat shock-induced Hsp72 induction across multiple cell lines, with 100% inhibition in MM.1S and MEF cells, 99% inhibition in CHO cells, and 85% inhibition in PC-3 cells[1].
NSC-134754 (2 μM; 5 h pre-incubation, present during overnight Velcade treatment) completely inhibits proteasome inhibitor (Velcade)-induced Hsp72 induction in MM.1S cells[1].
NSC-134754 (2 μM; 5 h pre-incubation, present during overnight radicicol treatment) inhibits Hsp90 inhibitor (radicicol)-induced Hsp72 induction by 90% in MM.1S cells[1].
NSC-134754 (2 μM; during proteasome inhibitor treatment) inhibits proteasome inhibitor (MG132)-induced Hsp72 induction by 90% in PC-3 cells[1].
NSC-134754 (2 μM; during Hsp90 inhibitor treatment) inhibits Hsp90 inhibitor (17-AAG)-induced Hsp72 induction by 70% in PC-3 cells[1].
NSC-134754 (2 μM; 5 h pre-incubation, present during 48 h radicicol treatment) sensitizes MM.1S multiple myeloma cells to Hsp90 inhibitor (Radicicol HY-N6769)-induced apoptosis, as measured by increased PARP cleavage[1].
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