Molecular structure of JNJ 26854165, CAS Number: 881202-45-5
JNJ 26854165 (CAS 881202-45-5)
Alternate Names:
Serdemetan; N1-(2-(1H-Indol-3-yl)ethyl)-N4-(pyridin-4-yl)benzene-1,4-diamine
Application:
JNJ 26854165 is a p53 activator and HDM2 ubiquitin ligase (MDM2) inhibitor
CAS Number:
881202-45-5
Purity:
≥98%
Molecular Weight:
328.41
Molecular Formula:
C21H20N4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
JNJ 26854165 is a tryptamine derivative which activates p53 and acts as an MDM2 (HDM2 ubiquitin ligase) inhibitor. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines. JNJ 26854165 is an MDM2 inhibitor which can inhibit the interaction of MDM2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of MDM2. A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells.
JNJ 26854165 (CAS 881202-45-5) References
- The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias. | Kojima, K., et al. 2010. Mol Cancer Ther. 9: 2545-57. PMID: 20736344
- Small-molecule inhibitors of p53-MDM2 interaction: the 2006-2010 update. | Millard, M., et al. 2011. Curr Pharm Des. 17: 536-59. PMID: 21391905
- Novel targeted therapeutics: inhibitors of MDM2, ALK and PARP. | Yuan, Y., et al. 2011. J Hematol Oncol. 4: 16. PMID: 21504625
- Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program. | Smith, MA., et al. 2012. Pediatr Blood Cancer. 59: 329-32. PMID: 21922647
- Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts. | Chargari, C., et al. 2011. Cancer Lett. 312: 209-18. PMID: 21937165
- The novel anticancer agent JNJ-26854165 induces cell death through inhibition of cholesterol transport and degradation of ABCA1. | Jones, RJ., et al. 2013. J Pharmacol Exp Ther. 346: 381-92. PMID: 23820125
- Serdemetan antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes. | Lehman, JA., et al. 2013. PLoS One. 8: e74741. PMID: 24040331
- The novel anticancer agent JNJ-26854165 is active in chronic myeloid leukemic cells with unmutated BCR/ABL and T315I mutant BCR/ABL through promoting proteosomal degradation of BCR/ABL proteins. | You, L., et al. 2017. Oncotarget. 8: 7777-7790. PMID: 27999193
- Inhibitors of ubiquitin E3 ligase as potential new antimalarial drug leads. | Jain, J., et al. 2017. BMC Pharmacol Toxicol. 18: 40. PMID: 28577368
- Precision and recall oncology: combining multiple gene mutations for improved identification of drug-sensitive tumours. | Naulaerts, S., et al. 2017. Oncotarget. 8: 97025-97040. PMID: 29228590
- Proteomic investigating the cooperative lethal effect of EGFR and MDM2 inhibitors on ovarian carcinoma. | Chang, SJ., et al. 2018. Arch Biochem Biophys. 647: 10-32. PMID: 29655550
- Gain-of-Function Mutant TP53 R248Q Overexpressed in Epithelial Ovarian Carcinoma Alters AKT-Dependent Regulation of Intercellular Trafficking in Responses to EGFR/MDM2 Inhibitor. | Lai, ZY., et al. 2021. Int J Mol Sci. 22: PMID: 34445495
- Progress in Anticancer Drug Development Targeting Ubiquitination-Related Factors. | Li, Q. and Zhang, W. 2022. Int J Mol Sci. 23: PMID: 36499442
Inhibitor of:
ASB-11, CDIP, EG229862, hnRNP K, LYZL6, MDM2, p19 ARF, p53CSV, PHD (peptidyl-proline 4-dioxygenase), SIAH-2, and Trp53i13.Activator of:
BC030500, p53, p53AIP1, and PIG11.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
JNJ 26854165, 5 mg | sc-364514 | 5 mg | $168.00 | |||
JNJ 26854165, 25 mg | sc-364514A | 25 mg | $566.00 |