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E1 E2 E3 Enzyme

E1 E2 E3 Enzyme

A protein modifier called ubiquitin (UB) controls a variety of vital cellular functions. The E1 enzyme activates UB's C-terminal carboxylate to start the process of UB's transfer through the E1-E2-E3 cascade onto target proteins. The ubiquitin is attached to the E1 enzyme by a thioester bond during an ATP-dependent reaction, and this enzyme serves as the activating enzyme. The ubiquitin is transferred from the E1 enzyme to the conjugating E2 enzyme. The E3 enzyme, also known as the ubiquitin ligase, catalyzes the transfer of ubiquitin to the target protein (also known as the substrate) by forming an isopeptide bond.

E1 E2 E3 Enzyme related products

Structure Cat No. Product Name CAS No. Product Description
AMG 232 V3460 AMG 232 1352066-68-2 AMG 232 (AMG-232; AMG232) is a novel, potent, selective, orally bioavailable and piperidinone-based inhibitor of MDM2-p53 protein-protein interaction with anticancer activity.
Antitumor agent-153 V87388 Antitumor agent-153 Antitumor agent-153 (compound 11b) is an optimized H2A histone ubiquitination inhibitor based on PRT4165.
Antitumor agent-81 V73099 Antitumor agent-81 2765180-17-2 Antitumor agent-81 (compound 5 a) is a low cytotoxic P62-RNF168 agonist that promotes the interaction between P62 and RNF168.
BC-1293 V99658 BC-1293 1219395-86-4 BC-1293 is an inhibitor of the E3 ligase subunit FBXO24.
BC-1382 V73094 BC-1382 1013753-99-5 BC-1382 is a potent inhibitor of ubiquitin E3 ligase HECTD2 that specifically disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).
BC-1901S V87394 BC-1901S 1358617-36-3 BC-1901S is a proteasome-independent NRF2 activator and stabilizer.
BIO-2007817 V93035 BIO-2007817 BIO-2007817 is a positive allosteric modulator (PAM) of Parkin, an E3 ligase.
Brigimadlin (BI 907828) V73090 Brigimadlin (BI 907828) 2095116-40-6 Brigimadlin (BI 907828) is an inhibitor (blocker/antagonist) of the E3 ubiquitin protein ligase MDM-2.
Cbl-b-IN-10 V73102 Cbl-b-IN-10 2815225-12-6 Cbl-b-IN-10 (Compound 463) is an inhibitor (blocker/antagonist) of casitas b lineage lymphoma (Cbl-b) and c-Cbl? with IC50 of 6.0 nM and 3.5 nM respectively.
Cbl-b-IN-11 V73114 Cbl-b-IN-11 2815225-15-9 Cbl-b-IN-11 (Compound 466) is an inhibitor (blocker/antagonist) of casitas b lineage lymphoma (Cbl-b) and c-Cbl with IC50 of 6.4 nM and 6.1 nM respectively.
Cbl-b-IN-12 V73110 Cbl-b-IN-12 2851871-29-7 Cbl-b-IN-12 (Example 10) is a casitas b-lineage lymphoma (CBL-B) inhibitor (antagonist) with IC50 of <100 nM.
Cbl-b-IN-13 V73107 Cbl-b-IN-13 2368841-85-2 Cbl-b-IN-13 (Example 520) is a Cbl-b inhibitor (antagonist) with IC50 of <100 nM.
Cbl-b-IN-15 V78678 Cbl-b-IN-15 Cbl-b-IN-15 (compound 25) is an inhibitor (blocker/antagonist) of the RING finger E3 ligase Cbl (IC50= 15 nM).
Cbl-b-IN-16 V83801 Cbl-b-IN-16
Cbl-b-IN-17 V87387 Cbl-b-IN-17 Cbl-b-IN-17 (Example-40) is an inhibitor of Cbl-b with IC50 value <100 nM.
Cbl-b-IN-18 V87389 Cbl-b-IN-18 Cbl-b-IN-18 (compound 51) is an inhibitor of the E3 ubiquitin ligase Cbl-b, inhibiting Cbl-b phosphorylation (IC50< 100 nM).
Cbl-b-IN-19 V87390 Cbl-b-IN-19 Cbl-b-IN-19 (Compound 49) is an inhibitor of the RING finger E3 ligase Cbl-b, inhibits Cbl-b phosphorylation with IC50 < 100 nM.
Cbl-b-IN-20 V87392 Cbl-b-IN-20 Cbl-b-IN-20 (Example 50) is a casitas B-lineage lymphoma oncogene-b (Cbl-b) inhibitor with IC50 value <100 nM.
Cbl-b-IN-26 V98538 Cbl-b-IN-26 3035443-17-2 Cbl-b-IN-26 (Example A1) is an inhibitor of Cbl-b with a Kd of 34.6 nM.
Cbl-b-IN-6 V73103 Cbl-b-IN-6 2815221-33-9 Cbl-b-IN-6 (Compound 246) is an inhibitor (blocker/antagonist) of casitas b lineage lymphoma (Cbl-b) and c-Cbl? with IC50 of 5.8 nM and 4.4 nM respectively.
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