NSC-134754
NSC-134754 (NZ-28) is a dehydroemetine derivative and heat shock protein (HSP) 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 can be used for the research of multiple myeloma, prostate carcinoma, colon carcinoma.
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- CAS No.: 75041-32-6
- Formule: C27H34N2O2
- Masse moléculaire:418.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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) partially inhibits HSF-1-dependent transcription (40% reduction) in heat-shocked PC-3 cells[1].
NSC-134754 (2 μM; 5 h pre-incubation) does not inhibit heat shock-induced Hsp72 mRNA transcription in PC-3 cells[1].
NSC-134754 (2 μM) 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) completely inhibits proteasome inhibitor (Velcade)-induced Hsp72 induction in MM.1S cells[1].
NSC-134754 (2 μM; 5 h) inhibits Hsp90 inhibitor (radicicol)-induced Hsp72 induction by 90% in MM.1S cells[1].
NSC-134754 (2 μM) inhibits proteasome inhibitor (MG132)-induced Hsp72 induction by 90% in PC-3 cells[1].
NSC-134754 (2 μM) inhibits Hsp90 inhibitor (17-AAG)-induced Hsp72 induction by 70% in PC-3 cells[1].
NSC-134754 (2 μM; 5 h pre-incubation) 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. Further protocols information, click here.
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Cell Line:CHO cells
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Concentration:1 μM; 2 μM
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Incubation Time:16 h (prior to heat shock)
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Result:Strongly inhibited heat shock-induced Hsp72 induction at 1 μM.
Completely inhibited heat shock-induced Hsp72 induction at 2 μM.
Chemical Information
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CAS No. 75041-32-6
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Masse moléculaire 418.57
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Formule C27H34N2O2
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SMILES
COC1=C(C=C(C2=C1)CCN3CC(CC)=C(C[C@]32[H])C[C@H]4NCCC5=C4C=CC=C5)OC
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Synonyms
NZ-28
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NSC-134754 Related Classifications
HY-123303 Related Classifications
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