CEP-1612
CEP-1612 is a proteasome inhibitor responsible for the proteolysis of important cell cycle and apoptosis-regulatory proteins. CEP-1612 helps to induce p21WAF1 and p27KIP1 expression and apoptosis and inhibits tumor growth of the human lung cancer. CEP1612 is a promising candidate for further development as an anticancer drug and demonstrate the feasibility of using proteasome inhibitors as novel antitumor agents.
1: Kazi A, Sun J, Doi K, Sung SS, Takahashi Y, Yin H, Rodriguez JM, Becerril J, Berndt N, Hamilton AD, Wang HG, Sebti SM. The BH3 alpha-helical mimic BH3-M6 disrupts Bcl-X(L), Bcl-2, and MCL-1 protein-protein interactions with Bax, Bak, Bad, or Bim and induces apoptosis in a Bax- and Bim-dependent manner. J Biol Chem. 2011 Mar 18;286(11):9382-92. doi: 10.1074/jbc.M110.203638. Epub 2010 Dec 9. PubMed PMID: 21148306; PubMed Central PMCID: PMC3059047.
2: Kim WY, Horbinski C, Sigurdson W, Higgins D. Proteasome inhibitors suppress formation of polyglutamine-induced nuclear inclusions in cultured postmitotic neurons. J Neurochem. 2004 Dec;91(5):1044-56. PubMed PMID: 15569248.
3: Sun J, Nam S, Lee CS, Li B, Coppola D, Hamilton AD, Dou QP, Sebti SM. CEP1612, a dipeptidyl proteasome inhibitor, induces p21WAF1 and p27KIP1 expression and apoptosis and inhibits the growth of the human lung adenocarcinoma A-549 in nude mice. Cancer Res. 2001 Feb 15;61(4):1280-4. PubMed PMID: 11245420.
4: Kitson RP, Lu M, Siman R, Goldfarb RH. Proteasome inhibitor and lymphocyte function: partial inhibition of cell-mediated cytotoxicity and implication that the lymphocyte proteasome may contain multiple chymotryptic domains. In Vivo. 2000 Jan-Feb;14(1):265-8. PubMed PMID: 10757085.
5: An B, Goldfarb RH, Siman R, Dou QP. Novel dipeptidyl proteasome inhibitors overcome Bcl-2 protective function and selectively accumulate the cyclin-dependent kinase inhibitor p27 and induce apoptosis in transformed, but not normal, human fibroblasts. Cell Death Differ. 1998 Dec;5(12):1062-75. PubMed PMID: 9894613.
2: Kim WY, Horbinski C, Sigurdson W, Higgins D. Proteasome inhibitors suppress formation of polyglutamine-induced nuclear inclusions in cultured postmitotic neurons. J Neurochem. 2004 Dec;91(5):1044-56. PubMed PMID: 15569248.
3: Sun J, Nam S, Lee CS, Li B, Coppola D, Hamilton AD, Dou QP, Sebti SM. CEP1612, a dipeptidyl proteasome inhibitor, induces p21WAF1 and p27KIP1 expression and apoptosis and inhibits the growth of the human lung adenocarcinoma A-549 in nude mice. Cancer Res. 2001 Feb 15;61(4):1280-4. PubMed PMID: 11245420.
4: Kitson RP, Lu M, Siman R, Goldfarb RH. Proteasome inhibitor and lymphocyte function: partial inhibition of cell-mediated cytotoxicity and implication that the lymphocyte proteasome may contain multiple chymotryptic domains. In Vivo. 2000 Jan-Feb;14(1):265-8. PubMed PMID: 10757085.
5: An B, Goldfarb RH, Siman R, Dou QP. Novel dipeptidyl proteasome inhibitors overcome Bcl-2 protective function and selectively accumulate the cyclin-dependent kinase inhibitor p27 and induce apoptosis in transformed, but not normal, human fibroblasts. Cell Death Differ. 1998 Dec;5(12):1062-75. PubMed PMID: 9894613.
| Chemical | |
|---|---|
| CAS Num | 189036-01-9 |
| Chemical Formula | C35H53N7O7 |
| Molecular Weight | 683.84 |
| IUPAC Chemical Name | 2H-Isoindole-2-decanamide, alpha-cyclopentyl-N-((1S)-1-((((1S)-1-formyl-3-methylbutyl)amino)carbonyl)-4-((imino(nitroamino)methyl)amino)butyl)-1,3-dihydro-1,3-dioxo- |
| Exact Mass | 683.40065 |
| Elemental Analysis | C, 61.47; H, 7.81; N, 14.34; O, 16.38 |
| Synonym | CEP-1612; CEP 1612; CEP1612; UNII-9K6U075027. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | CC(C)C[C@@H](C=O)NC(=O)[C@H](CCCNC(=N)N[N+](=O)[O-])NC(=O)C(CCCCCCCCN1C(=O)c2ccccc2C1=O)C3CCCC3 |
| Biological | |
| Targets and Effects | proteasome inhibitor |
| Pathways | Apoptosis |
| Physical | |
| 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). |
| Shelf Life | >2 years if stored properly |
Mailing Address
Anba Pharma Company
3-H Gill Street, Suite 300
Woburn, MA 01801
United State
Our Contact Info.
Tel: 1+610-883-0668
Email: sales@AnbaPharma.com