WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H407131
CAS#: 75041-32-6
Description: NZ28, also known as NSC134754, is potent HSF1 inhibitor, which induced inhibition of HSF1, SP1 and NF-κB triggers the loss of the natural killer cell-activating ligands MICA/B on human tumor cells. Heat-shock transcription factor HSF1 has a critical role in human epidermal growth factor receptor-2-induced cellular transformation and tumorigenesis.
Hodoodo Cat#: H407131
Name: NZ-28
CAS#: 75041-32-6
Chemical Formula: C27H34N2O2
Exact Mass: 418.26
Molecular Weight: 418.580
Elemental Analysis: C, 77.48; H, 8.19; N, 6.69; O, 7.64
Synonym: NZ-28; NZ28; NZ 28; NSC 134754; NSC 134754; NSC134754.
IUPAC/Chemical Name: (S)-3-ethyl-9,10-dimethoxy-2-(((R)-1,2,3,4-tetrahydroisoquinolin-1-yl)methyl)-1,6,7,11b-tetrahydro-4H-pyrido[2,1-a]isoquinoline
InChi Key: HDIJLRXRAJUXQB-RPBOFIJWSA-N
InChi Code: InChI=1S/C27H34N2O2/c1-4-18-17-29-12-10-20-15-26(30-2)27(31-3)16-23(20)25(29)14-21(18)13-24-22-8-6-5-7-19(22)9-11-28-24/h5-8,15-16,24-25,28H,4,9-14,17H2,1-3H3/t24-,25+/m1/s1
SMILES Code: COC1=C(OC)C=C(CCN2CC(CC)=C(C[C@H]3NCCC4=C3C=CC=C4)C[C@]25[H])C5=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 418.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Schilling D, Kühnel A, Tetzlaff F, Konrad S, Multhoff G. NZ28-induced inhibition of HSF1, SP1 and NF-κB triggers the loss of the natural killer cell-activating ligands MICA/B on human tumor cells. Cancer Immunol Immunother. 2015 May;64(5):599-608. doi: 10.1007/s00262-015-1665-9. Epub 2015 Feb 18. PubMed PMID: 25854583; PubMed Central PMCID: PMC4412431.
2: Schilling D, Kühnel A, Konrad S, Tetzlaff F, Bayer C, Yaglom J, Multhoff G. Sensitizing tumor cells to radiation by targeting the heat shock response. Cancer Lett. 2015 May 1;360(2):294-301. doi: 10.1016/j.canlet.2015.02.033. Epub 2015 Feb 23. PubMed PMID: 25721082.
3: Kudriavtsev VA, Makarova IuM, Kabakav AE. [Thermosensitization of tumor cells with inhibitors of chaperone activity and expression]. Biomed Khim. 2012 Nov-Dec;58(6):662-72. Russian. PubMed PMID: 23350198.
4: Meng L, Gabai VL, Sherman MY. Heat-shock transcription factor HSF1 has a critical role in human epidermal growth factor receptor-2-induced cellular transformation and tumorigenesis. Oncogene. 2010 Sep 16;29(37):5204-13. doi: 10.1038/onc.2010.277. Epub 2010 Jul 12. PubMed PMID: 20622894; PubMed Central PMCID: PMC2940982.
5: Zaarur N, Gabai VL, Porco JA Jr, Calderwood S, Sherman MY. Targeting heat shock response to sensitize cancer cells to proteasome and Hsp90 inhibitors. Cancer Res. 2006 Feb 1;66(3):1783-91. PubMed PMID: 16452239.
6: Seppo A, Moreland M, Schweingruber H, Tiemeyer M. Zwitterionic and acidic glycosphingolipids of the Drosophila melanogaster embryo. Eur J Biochem. 2000 Jun;267(12):3549-58. PubMed PMID: 10848971.