E3 Ligase

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1029 Lenalidomide (CC-5013) <1 mg/mL 52 mg/mL <1 mg/mL
S1567 Pomalidomide <1 mg/mL 54 mg/mL '<1 mg/mL
S1193 Thalidomide <1 mg/mL 51 mg/mL 2 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
S5315 PRT4165 <1 mg/mL 11 mg/mL 4 mg/mL
S8760 Iberdomide(CC220) <1 mg/mL 90 mg/mL 7 mg/mL
S7892 Avadomide(CC-122) <1 mg/mL 57 mg/mL 1 mg/mL
S2678 NSC 207895 <1 mg/mL 0.4 mg/mL <1 mg/mL
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
S8888 GMB-475 <1 mg/mL 100 mg/mL 50 mg/mL
S6794 Thalidomide-O-COOH (Cereblon ligand 3) <1 mg/mL 66 mg/mL <1 mg/mL

E3 Ligase 製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1029

Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase.

S1567

Pomalidomide

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.

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.

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.

S8760

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.

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 CRL4CRBN.

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.

S8888

GMB-475

GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.

S6794

Thalidomide-O-COOH (Cereblon ligand 3)

Thalidomide-O-COOH (Cereblon ligand 3), a Thalidomide-based Cereblon (CRBN) ligand, is used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs (Proteolysis Targeting Chimera).

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1029

Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase.

S1567

Pomalidomide

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.

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.

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.

S8760

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.

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 CRL4CRBN.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

2020, 34(7-8):526-543

2018, 15(2):1673-1679

2016, 7(6):1140-1151

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

2020, 26(1):122-134

2020, 30(2):497-509

2020, 126:93-103

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.

2019, 36(2):179-193

2019, 36(2):179-193

2017, 18(1):40

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S8888

GMB-475

GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.

S6794

Thalidomide-O-COOH (Cereblon ligand 3)

Thalidomide-O-COOH (Cereblon ligand 3), a Thalidomide-based Cereblon (CRBN) ligand, is used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs (Proteolysis Targeting Chimera).

Tags: Ubiquitin ligase inhibitor | E3 ligase inhibitor