NSC-134754  (Synonyms: NZ-28)

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].

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].

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

418.57

C₂₇H₃₄N₂O₂

75041-32-6

COC1=C(C=C(C2=C1)CCN3CC(CC)=C(C[C@]32[H])C[C@H]4NCCC5=C4C=CC=C5)OC

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zaarur N, et al. Targeting heat shock response to sensitize cancer cells to proteasome and Hsp90 inhibitors. Cancer Res. 2006;66(3):1783-1791.  [Content Brief]