| DC11922 |
BC-1382 |
A potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction with IC50 of 5 nM. |
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| DC9269 |
PRT4165（NSC-600157）
Featured
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PRT4165 is a potent inhibitor of PRC1 (Polycomb-repressive complex 1)-mediated H2A ubiquitylation. |
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| DC10710 |
Skp2 Inhibitor C1(SKPin C1)
Featured
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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. |
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| DC12349 |
TAME hydrochloride |
TAME hydrochloride is an inhibitor of anaphase-promoting complex (APC), which prevents its activation by Cdc20 and Cdh1. |
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| DC44890 |
Cbl-b-IN-1 |
Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC50 <100 nM. |
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| DC47192 |
RB-3 |
RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM. |
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| DC47677 |
NSC232003 |
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. |
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| DC48077 |
5-amino-2,4-dimethylpyridine (5A-DMP) |
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. |
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| DC48890 |
DCN1-UBC12-IN-2 |
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. |
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| DC48938 |
DCN1-UBC12-IN-1 |
DCN1-UBC12-IN-1 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.86 nM. Anticardiac fibrotic effect. |
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| DC49105 |
DCN1-UBC12-IN-3 |
DCN1-UBC12-IN-3 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.25 nM. Anticardiac fibrotic effect. |
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| DC50218 |
Keap1-Nrf2-IN-4 |
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. |
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| DC70100 |
MyoMed-205 |
MyoMed-205 is a small moelcule that inhibits MuRF1 (TRIM63) activity and MuRF1/MuRF2 expression. |
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| DC70103 |
MS.001
Featured
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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). |
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| DC70254 |
BIO-2007817 |
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. |
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| DC70324 |
CRL inhibitor 33-11 |
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. |
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| DC70538 |
KH-4-43 |
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. |
|
| DC70632 |
Myomed-946 |
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. |
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| DC72773 |
Brigimadlin
Featured
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Brigimadlin is an E3 ubiquitin-protein ligase MDM-2 inhibitor. Brigimadlin serves as an antineoplastic agent. |
|
| DC74297 |
AAA237 |
AAA-237 (AAA237) is a small molecule Skp2 E3 ligase inhibitor, binds to Skp2 protein (KD=28.77 uM) and inhibits the degradation of Skp2 substrates, inhibits the proliferation of the NSCLC cells. |
|
| DC74298 |
BC18630 |
BC18630 (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays. |
|
| DC74299 |
BC18630 free base |
BC18630 free base (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays. |
|
| DC74300 |
BC18813 |
BC18813 (BC 18813) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 48 nM in cell-based assays. |
|
| DC74301 |
NX-1607
Featured
|
NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research. |
|
| DC74302 |
MN551 |
MN551 is a Cys111-specific, covalent ligand targeting the E3 ligase SOCS2 with ITC Ki value of 2.2 uM, blocks recruitment of cellular SOCS2 protein to its native substrate. |
|
| DC74303 |
MN714 |
MN714 is a cell-premeable prodrug of MN551 containing a pivaloyloxymethyl (POM) and covalent inhibitor of E3 ligase suppressor of cytokine signaling 2 (SOCS2). |
|
| DC74305 |
Skp2-2 |
Skp2-2 is a small molecule inhibitor of Skp2-Cks1 interaction with IC50 of 27.8 uM, significantly and dose-dependently reduces the protein expression of Skp2 in cancer cells. |
|
| DC74306 |
T0467 |
T0467 is a small molecule activator of PINK1-Parkin signaling, activates Parkin mitochondrial translocation in dopaminergic neurons and myoblasts (20 uM, 3h), does not induce mitochondrial accumulation of PINK1. |
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