E3 Ligase

  • Compare E3 Ligase Products
  • Research Area

E3 Ligase Inhibitors | Activators | Antagonists (8)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1061 Nutlin-3 Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.
  • Hepatology, 2015, 62(5):1497-510
  • Mol Ther, 2015, 23(5):857-65
  • Int J Cancer, 2014, 10.1002/ijc.29194
S1172 JNJ-26854165 (Serdemetan) JNJ-26854165 (Serdemetan) 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 1.
  • Sci Rep, 2014, 4:4664
  • Mol Ther, 2015, 23(5):857-65
  • Head Neck, 2014, 10.1002/hed.23822
S1193 Thalidomide Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.
  • FASEB J, 2015, 29(12):4829-39
S2678 NSC 207895 NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.
S2225 TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
S2754 AT406 (SM-406, ARRY-334543) AT406 (SM-406, ARRY-334543) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.
  • Cancer Res, 2015, 10.1158/0008-5472.CAN-14-2199
  • Int J Oncol, 2016, 10.3892/ijo.2016.3525. Epub 2016 May 16
S2781 RITA (NSC 652287) RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.
  • Nat Chem Biol, 2015, 10.1038/nchembio.1986
  • Oncogene, 2014, 10.1038/onc.2014.37
S8000 Tenovin-1 Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2.

Hover Mouse over '+' to display IC50

Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1061 Nutlin-3 <1 mg/mL 100 mg/mL 30 mg/mL
S1172 JNJ-26854165 (Serdemetan) <1 mg/mL 66 mg/mL 2 mg/mL
S1193 Thalidomide <1 mg/mL 52 mg/mL 2 mg/mL
S2678 NSC 207895 <1 mg/mL 0.4 mg/mL <1 mg/mL
S2225 TAME 69 mg/mL 69 mg/mL 3 mg/mL
S2754 AT406 (SM-406, ARRY-334543) <1 mg/mL 100 mg/mL 100 mg/mL
S2781 RITA (NSC 652287) <1 mg/mL 58 mg/mL 8 mg/mL
S8000 Tenovin-1 <1 mg/mL 74 mg/mL <1 mg/mL
Tags: Ubiquitin ligase inhibitor | E3 ligase inhibitor
Contact Us