For research use only. We do not sell to patients.

Serdemetan

CAS No. : 881202-45-5

Biological Activity：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.
IC50 value: HDM2 ubiquitin ligase
Target:
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-null-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.

Research Area：Cancer

Targets：MDM-2/p53|Apoptosis|E1/E2/E3 Enzyme

Related Screening Libraries:Clinical Compound Library Plus;Bioactive Compound Library Plus;Apoptosis Compound Library;Metabolism/Protease Compound Library;Anti-Cancer Compound Library;Clinical Compound Library;Autophagy Compound Library;Anti-Aging Compound Library; Oxygen Sensing Compound Library;Ubiquitination Compound Library;Ferroptosis Compound Library;Pyroptosis Compound Library;Glutamine Metabolism Compound Library;Anti-Pancreatic Cancer Compound Library;Anti-Blood Cancer Compound Library;Anti-Cancer Metabolism Compound Library;Transcription Factor-Targeted Library;Anti-Liver Cancer Compound Library ;Anti-Colorectal Cancer Compound Library ;Protein-protein Interaction Inhibitor Library;

Related Small Molecules:Physalin A;Bomedemstat ditosylate;Enpp/Carbonic anhydrase-IN-1;GK563;Calpeptin;Lobetyolin;UBE2T/FANCL-IN-1;BJE6-106;Dinaciclib;Ecteinascidin 770;MDM2-p53-IN-15;AT9283;Staurosporine;SNS-032;C188-9;ZLDI-8;Topoisomerase I/II inhibitor 3;Xevinapant;Mangiferin;Cambinol;Antioxidant agent-5;Apoptosis inducer 9;Bafetinib;Cyclovirobuxine D

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

About Us:

• MedChemExpress (MCE) offers a wide range of high-quality research chemicals and biochemicals (novel life-science reagents, reference compounds and natural compounds) for scientific use；
• Structurally and synthetically diverse biologically active compounds；
•  roduct quality is the key to our success and we take pride in offering only the highest-grade products.；
• We provide HNMR, LC-MS, HPLC, stability testing and activity assays of our products to clients.；
• Product identity, quality, purity and activity are assured by our robust quality control programs and procedures.；

Structurally and synthetically diverse biologically active compounds；

• Customized order volume ranging from milligrams to kilograms scale；

We provide customer-oriented services. To explore more, please contact us at [email protected]. Our team will gladly assist you.