E3 Ligase

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
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
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
S2754 AT406 (SM-406) <1 mg/mL 100 mg/mL 100 mg/mL
Catalog No. Information Product Use Citations Product Validations
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.

S2225

TAME

Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.

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.

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.

S2754

AT406 (SM-406)

AT406 (SM-406) 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.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

S2225

TAME

Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.

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.

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.

S2754

AT406 (SM-406)

AT406 (SM-406) 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.

Catalog No. Information Product Use Citations Product Validations
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.

Catalog No. Information Product Use Citations Product Validations
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.

2015, 62(5):1497-510

2015, 23(5):857-65

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.

2014, 4:4664

2015, 23(5):857-65

2014, 10.1002/hed.23822

Tags: Ubiquitin ligase inhibitor | E3 ligase inhibitor