A potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction with IC50 of 5 nM.

CC-122 is a novel agent for DLBCL with antitumor and immunomodulatory activity.CC-122 binds CRBN and degrades Aiolos and Ikaros resulting in a mimicry of IFN signaling and apoptosis in DLBCL.

Iberdomide (CC-220) is a cereblon modulator in clinical development for systemic lupus erythematosis. Iberdomide exhibits an IC50 of 60 nM in TR-FRET cereblon binding assay.

PRT4165 is a potent inhibitor of PRC1 (Polycomb-repressive complex 1)-mediated H2A ubiquitylation.

Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.

TAME hydrochloride is an inhibitor of anaphase-promoting complex (APC), which prevents its activation by Cdc20 and Cdh1.

Tasisulam sodium is The sodium salt of an acyl-sulfonamide with potential antineoplastic activity.

Mezigdomide is a cereblon E3 ubiquitin ligase modulating agent with potential immunomodulating and antineoplastic activities. Mezigdomide specifically binds to cereblon (CRBN), thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins for ubiquitination. This induces proteasome-mediated degradation of certain transcription factors, some of which are transcriptional repressors in T cells. This leads to modulation of the immune system, including activation of T lymphocytes, and downregulation of the activity of other proteins, some of which play key roles in the proliferation of certain cancer cell types.

Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC50 <100 nM.

RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM.

NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor that binds to the 5mC binding pocket of the SRA domain of UHRF1. NSC232003 modulates DNA methylation in a cellular context.

5-amino-2,4-dimethylpyridine (5A-DMP) is a novel tandem Tudor domain (TTD)-binding compound that inhibits the full-length UHRF1:LIG1 interaction in Xenopus egg extracts.

DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation.

DCN1-UBC12-IN-1 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.86 nM. Anticardiac fibrotic effect.

DCN1-UBC12-IN-3 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.25 nM. Anticardiac fibrotic effect.

Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity.

MyoMed-205 is a small moelcule that inhibits MuRF1 (TRIM63) activity and MuRF1/MuRF2 expression.

MS.001 is a small molecule that inhibits both the chaperone binding and ubiquitin ligase activity of C-terminus of Hsc70 interacting protein (CHIP) at low micromolar concentrations (IC50=3.3 uM).

BIO-2007817 is a small-molecule positive allosteric modulator of Parkin E3 ligase with EC50 of 0.17 uM (TR-FRET).BIO-2007817 stimulated Parkin autoubiquitination as measured by Western blots in a concentration-dependent manner, was also able to induce the appearance of monoubiquitinated forms of Miro1.BIO-2007817 induced the appearance of slower-migrating Parkin species in a concentration-dependent manner with maximal efficacy at 20 uM in Parkin autoubiquitination assay.BIO-2007817 does not affect the rate of Parkin translocation to mitochondria nor the number of mitochondria within lysosomes.

CRL inhibitor 33-11 is a small moelcule E3 CRL inhibitor, directly and selectively binds to the purified E3 ROC1-CUL4A CTD and ROC1-CUL1 CTD complex with Kd of 0.223 and 4.53 uM, respecitvely.CRL inhibitor 33-11 binds to ROC1-CUL1 more effectively than ROC1-CUL1-Nedd8.CRL inhibitor 33-11 showed the ability to inhibit ubiquitination by ROC1–CUL1 more potently than that by ROC1-CUL1-Nedd8.CRL inhibitor 33-11 inhibited the ubiquitination of CK1α by CRL4CRBN in vitro.

KH-4-43 is a small moelcule E3 CRL4 inhibitor and exhibits antitumor potential, directly and selectively binds to the purified E3 ROC1-CUL4A CTD complex with Kd of 83 nM.KH-4-43 weakly binds to the purified, highly related E3 ROC1-CUL1 CTD complex with Kd of 9.4 uM, >100-fold less potent than ROC1-CUL4A CTD, showed little effect on Ub thiol ester formation with E1/E2 Cdc34.KH-4-43 inhibited the ubiquitination of CK1α by CRL4CRBN in vitro. Treatment of cells with KH-4-43 caused accumulation of the E3 CRL4 substrate CDT1.KH-4-43 inhibited cell viability against a panel of tumor lines, NB-4, MV4-11, OVCAR-3, and CAPAN-2 cell with IC50 of 1.8, 3.0, 3.9, and 4.8 uM, respectively.KH-4-43 suppress the growth of human tumor xenografts in mice.

MyoMed-946 is a small moelcule that inhibits MuRF1 (TRIM63) activity and MuRF1/MuRF2 expression; MyoMed-946 inhibits MuRF1 expression/activity in vivo and is able to attenuate skeletal muscle atrophy and dysfunction in mice treated with monocrotaline to induce right ventricular hypertrophy and subsequent cardiac cachexia. MyoMed-946 attenuates skeletal muscle strength loss in mouse model for type 2 diabetes mellitus (T2DM), with no significant effects on serum glucose. MyoMed-946 attenuates induction of MuRF1 in tumor stressed muscles. MyoMed-946 also rescues citrate synthase and complex-1 activities in tumor-stressed muscles. MuRF1 (muscle-specific RING finger protein-1) is a muscle-specific ubiquitin ligase that regulates muscle catabolism during chronic wasting states, both MuRF1 and MuRF2 participate in glucose and, also, in lipid regulation.