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10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Cited in 1 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
Serdemetan (JNJ-26854165) Serdemetan (JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase
In vitro
JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. 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 is an oral 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--HCT116.
In vivo
JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks.
Cell Data
cell lines:
Concentrations:0-10 μM
Incubation Time:72 hours
Powder Purity:≥99%
| Isomeric SMILES | C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4 |
|---|---|
| PubChem CID | 11609586 |
| Molecular Weight | 328.42 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| 1. Yanli Zhang, Yulin Zhang, Ye Lei, Junrong Wu, Yiyuan Kang, Shuo Zheng, Longquan Shao. (2023) MDM2 upregulation induces mitophagy deficiency via Mic60 ubiquitination in fetal microglial inflammation and consequently neuronal DNA damage caused by exposure to ZnO-NPs during pregnancy. JOURNAL OF HAZARDOUS MATERIALS, [PMID:37315416] [10.1016/j.jhazmat.2023.131750] |