E3 Ligase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

E3 Ligase Products

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.	Biomed Pharmacother, 2019, 116:109011 Eur J Pharmacol, 2019, 856:172409 J Immunol Res, 2018, 2018:5070573	(E) MM.1S cells were treated with Thal(Thalidomide) or Pom for 48 hours. In each case, western blot was carried out using cell lysates and the indicated Abs.
S2225	TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.		Knockdown of p21 or inhibiting APC/C by TAME sensitized NSCLC cells to 5-FU. Cells were treated with 5-FU. 2 days after treatment, surviving cells were stained with cystal violet. Representive microscopic fields were shown. The blue stained cells were counted and shown in histogram at the right side.
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.	Cancer Cell, 2019, 35(2):191-203 Nat Chem Biol, 2015, 10.1038/nchembio.1986 Oncogene, 2014, 10.1038/onc.2014.37	To determine the number of viable cells, cells were serum starved for 8 hours and treated with 25 nM RITA and stimulated with 1ug/mL SDF1α for 48 hours in serum-free media. After 48 hours, cells were harvested and counted by trypan blue exclusion, using standard methods.
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.	J Transl Med, 2019, 17(1):76	The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
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 K_i 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 Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Cell Chem Biol, 2019, 26(3):331-339	G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting.
S5315	PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.
S7892	Avadomide(CC-122) Avadomide(CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4^CRBN.
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.	Oncol Lett, 2018, 15(2):1673-1679 Stem Cell Reports, 2016, 7(6):1140-1151	Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).
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.	Cell Death Differ, 2019, 10.1038/s41418-019-0338-1 Oncogene, 2019, 38(14):2501-2515 Oncol Rep, 2019, 41(2):1075-1082	Ubiquitination of p53 in vivo by BIRC6 in the presence of Nutlin-3. Cells were treated with Nutlin-3 (20 uM, 24 h) before harvest. Cell lysates were immunoprecipitated with anti-p53 antibody and immunoblotted by anti-ubiquitin antibody.
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.	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 BMC Pharmacol Toxicol, 2017, 18(1):40
S8760^New	Iberdomide(CC220) Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay.

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.	Biomed Pharmacother, 2019, 116:109011 Eur J Pharmacol, 2019, 856:172409 J Immunol Res, 2018, 2018:5070573	(E) MM.1S cells were treated with Thal(Thalidomide) or Pom for 48 hours. In each case, western blot was carried out using cell lysates and the indicated Abs.
S2225	TAME Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.		Knockdown of p21 or inhibiting APC/C by TAME sensitized NSCLC cells to 5-FU. Cells were treated with 5-FU. 2 days after treatment, surviving cells were stained with cystal violet. Representive microscopic fields were shown. The blue stained cells were counted and shown in histogram at the right side.
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.	Cancer Cell, 2019, 35(2):191-203 Nat Chem Biol, 2015, 10.1038/nchembio.1986 Oncogene, 2014, 10.1038/onc.2014.37	To determine the number of viable cells, cells were serum starved for 8 hours and treated with 25 nM RITA and stimulated with 1ug/mL SDF1α for 48 hours in serum-free media. After 48 hours, cells were harvested and counted by trypan blue exclusion, using standard methods.
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.	J Transl Med, 2019, 17(1):76	The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
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 K_i 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 Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Cell Chem Biol, 2019, 26(3):331-339	G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting.
S5315	PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.
S7892	Avadomide(CC-122) Avadomide(CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4^CRBN.

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.	Oncol Lett, 2018, 15(2):1673-1679 Stem Cell Reports, 2016, 7(6):1140-1151	Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).

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.

Oncol Lett, 2018, 15(2):1673-1679

Stem Cell Reports, 2016, 7(6):1140-1151

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.	Cell Death Differ, 2019, 10.1038/s41418-019-0338-1 Oncogene, 2019, 38(14):2501-2515 Oncol Rep, 2019, 41(2):1075-1082	Ubiquitination of p53 in vivo by BIRC6 in the presence of Nutlin-3. Cells were treated with Nutlin-3 (20 uM, 24 h) before harvest. Cell lysates were immunoprecipitated with anti-p53 antibody and immunoblotted by anti-ubiquitin antibody.
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.	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 BMC Pharmacol Toxicol, 2017, 18(1):40

Catalog No.

Information

Product Use Citations

Product Validations

S1061

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.

Cell Death Differ, 2019, 10.1038/s41418-019-0338-1

Oncogene, 2019, 38(14):2501-2515

Oncol Rep, 2019, 41(2):1075-1082

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.

Cell, 2019, 36(2):179-193

Cancer Cell, 2019, 36(2):179-193

BMC Pharmacol Toxicol, 2017, 18(1):40

Catalog No.	Information	Product Use Citations	Product Validations
S8760^New	Iberdomide(CC220) Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay.

Catalog No.

Information

Product Use Citations

Product Validations

S8760^New

Iberdomide(CC220)

Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay.

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E3 Ligase

Signaling Pathway Map

Research Area

Inhibitory Selectivity