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You are here:Home-Inhibitors & Agonists-Proteasome/Ubiquitin-E3 Ubiquitin Ligase

Request The Product List ofE3 Ubiquitin Ligase E3 Ubiquitin Ligase

Cat. No. Product Name CAS No. Information
GY10091

cIAP1 E3 ligase inhibitor D19

380640-76-6

cIAP1 E3 ligase inhibitor D19 (cIAP1 inhibitor D19) is a small-molecule inhibitor of E3 ligase activity of cIAP1, inhibits cIAP1 auto-ubiquitination with IC50 of 14.1 uM, shows no effect on autoubiquitination of BRCA1/BARD1; binds to the RING domain of cIAP1 and inhibits the E3 ligase activity of cIAP1 by interfering with the dynamics of its interaction with E2, inhibited cIAP1 autoubiquitination with all of the E2s (t UbcH5a/b/c, UbcH6, and Ubc13/Uev1a) that can mediate its activity; suppresses c-MYC oncogenic function and cancer cell proliferation by stabilizing MAD1 protein and promoting the degradation of c-MYC.

GY10092

cIAP1 E3 ligase inhibitor D19-14

cIAP1 E3 ligase inhibitor D19-14 (cIAP1 inhibitor D19-14) is an improved analog of D19, demonstrates significantly increased ability to inhibit cIAP1 autoubiquitination and reduce protein levels of c-MYC in vitro; D19-14 is more potent in inhibiting the proliferation of cancer cells than D19, D19-14 exhibits acceptable pharmacokinetics properties in vivo, effectively decreases the levels of c-MYC protein in tumors in cancer xenograft model.

GY10329

HS-152

2284548-09-8

HS-152 (HS152) is a specific small-molecule inhibitor of SMAD ubiquitin regulatory factor 1 (SMURF1), not only potently inhibits SMURF1-mediated RHOB degradation with IC50 of 3.2 uM, but also strongly blocks SMURF1-mediated RHOA and SMAD1 degradation (IC50 4.4 uM and 2.1 uM, respectively); inhibits both SMURF1 and SMURF2 catalytic activities, effectively inhibits protrusive activity in HEK293T cells and blocks TGFβ-induced epithelial-mesenchymal transition (EMT) in MDCK cells, similar to the effects on these processes caused by SMURF1 loss.

GY10374

HOIPIN-1

HOIPIN-1 (JTP-0819958, HOIP inhibitor-1) is a chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=2.8 uM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-kB pathway.

GY10375

HOIPIN-8

HOIPIN-8 (HOIP inhibitor-8) is a potent chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=11 nM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-kB pathway; suppresses the linear ubiquitination activity by recombinant LUBAC, displays 255-fold increased potency over that of HOIPIN-1 (JTP-0819958, IC50=2.8 uM); also shows 10-fold and 4-fold enhanced inhibitory activities on LUBAC- and TNF-a-induced NF-kB activation respectively, without cytotoxicity; HOIPIN-8 is a powerful tool to explore the physiological functions of LUBAC.

GY10567

NRX-252114

NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule enhancer of β-catenin-β-TrCP interaction, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM); NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with >1500-fold cooperativity, surpassing the affinity of WT doublyphosphorylated peptide in vitro, induces the degradation of an engineered mutant β-Catenin in a cellular system; inserts into a naturally occurring PPI interface, with contacts optimized for both the substrate and ligase within the same small molecule entity, which is distinct from PROTACs.

GY06680

BC-1382

1013753-99-5

BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction with IC50 of 5 nM; drastically increases PIAS1 protein level with IC50 of 100 nM and improves PIAS1 protein stability, with no effect on PIAS3, PIAS4, and HECTD2 protein levels; suppresses LPS-induced PIAS1 degradation and restores PIAS1 protein levels at 800 nM, and proinflammatory cytokines released by PBMCs; attenuates LPS- and Pseudomonas aeruginosa-induced lung inflammation

GY06643

Iberdomide

1323403-33-3

Iberdomide is a potent, next-generation modulator of cereblon E3 ubiquitin ligase with IC50 of 60 nM; exhibits significantly higher affinity than lenalidomide and pomalidomide (IC50=1.5 and 1.2 uM, respectively); reduces and degrades Aiolos and Ikaros protein levels (EC50=1 nM and 0.5 nM, respectively) and BAFF- and CD40L-induced proliferation, plasmablast differentiation, and IgG secretion in cellular degradation assay.

GY06637

BRD5529

1358488-78-4

BRD5529 is a small-molecule inhibitor that disrupts the interaction of CARD9-E3 ubiquitin ligase TRIM62 with IC50 of 8.6 uM; directly and selectively bind CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation of CARD9, and demonstrates cellular activity and selectivity in CARD9-dependent pathways, selectively inhibits Dectin-1- mediated CARD9 activation, while leaving LPS-activated signaling intact.

GY06613

BC-1215

1507370-20-8

BC-1215 (BC1215) is a potent, highly unique, selective E3 ligase F box component Fbxo3 inhibitor with IL1β IC50 of 0.9 ug/mL; inhibits the Fbxo3-TRAF activation pathway for cytokine release, increases immunoreactive Fbxl2 levels and reduces TRAF proteins, impairs Fbxo3 ubiquitination of Fbxl2 with IC50 of 0.1 uM in vitro ubiquitination assay; reversibly inhibits Fbxo3 to destabilize TRAF proteins, remarkably suppresses the majority of the Th1 panel cytokines including G-CSF, GM-CSF, GROα, I-309, IL1-α, IL1-β, IL1rα, IL-6, IL-12, IL-23, MIP-1α, MIP-1β and TNFα, in PBMCs; ameliorates the severity of viral pneumonia, septic shock, colitis, and cytokine-driven inflammation systemically in murine models.

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