For research use only. Not for therapeutic Use.
JNJ-26854165 (Cat No.: I005297) is an inhibitor that targets the HDM2 ubiquitin ligase, a protein involved in the degradation of p53, a critical tumor suppressor protein. In cells with functional p53, JNJ-26854165 acts as an antagonist, disrupting the HDM2-p53 interaction. This disruption leads to early apoptosis (programmed cell death), inhibits cell proliferation, and delays apoptosis in cells that lack functional p53. JNJ-26854165 shows promise in cancer therapy by restoring the activity of p53 and promoting cell death in cancer cells with wild-type p53 or dysfunctional p53 pathways. If you need to, please contact us in time, and we will reply to you as soon as possible within 24 hours.
| Catalog Number | I005297 |
| CAS Number | 881202-45-5 |
| Synonyms | 1-N-[2-(1H-indol-3-yl)ethyl]-4-N-pyridin-4-ylbenzene-1,4-diamine |
| Molecular Formula | C₂₁H₂₀N₄ |
| Purity | ≥95% |
| Target | Metabolic Enzyme/Protease |
| Solubility | DMSO ≥64mg/mL Water <1.2mg/mL Ethanol ≥1.8mg/mL |
| Storage | Store at -20°C |
| IC50 | HDM2 ubiquitin ligase |
| IUPAC Name | 1-N-[2-(1H-indol-3-yl)ethyl]-4-N-pyridin-4-ylbenzene-1,4-diamine |
| InChI | InChI=1S/C21H20N4/c1-2-4-21-20(3-1)16(15-24-21)9-14-23-17-5-7-18(8-6-17)25-19-10-12-22-13-11-19/h1-8,10-13,15,23-24H,9,14H2,(H,22,25) |
| InChIKey | CEGSUKYESLWKJP-UHFFFAOYSA-N |
| SMILES | C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4 |
| Reference | </br>1:Serdemetan antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes. Lehman JA, Hauck PM, Gendron JM, Batuello CN, Eitel JA, Albig A, Kadakia MP, Mayo LD.PLoS One. 2013 Sep 6;8(9):e74741. doi: 10.1371/journal.pone.0074741. eCollection 2013. PMID: 24040331 Free PMC Article</br>2:Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts. Chargari C, Leteur C, Angevin E, Bashir T, Schoentjes B, Arts J, Janicot M, Bourhis J, Deutsch E.Cancer Lett. 2011 Dec 22;312(2):209-18. doi: 10.1016/j.canlet.2011.08.011. Epub 2011 Aug 22. PMID: 21937165 </br>3:Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program. Smith MA, Gorlick R, Kolb EA, Lock R, Carol H, Maris JM, Keir ST, Morton CL, Reynolds CP, Kang MH, Arts J, Bashir T, Janicot M, Kurmasheva RT, Houghton PJ.Pediatr Blood Cancer. 2012 Aug;59(2):329-32. doi: 10.1002/pbc.23319. Epub 2011 Sep 15. PMID: 21922647 Free PMC Article</br>4:A phase I first-in-human pharmacokinetic and pharmacodynamic study of serdemetan in patients with advanced solid tumors. Tabernero J, Dirix L, Schöffski P, Cervantes A, Lopez-Martin JA, Capdevila J, van Beijsterveldt L, Platero S, Hall B, Yuan Z, Knoblauch R, Zhuang SH.Clin Cancer Res. 2011 Oct 1;17(19):6313-21. doi: 10.1158/1078-0432.CCR-11-1101. Epub 2011 Aug 10. PMID: 21831953 Free Article |
