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Request The Product List ofE3 Ubiquitin Ligase E3 Ubiquitin Ligase

Cat. No. Product Name CAS No. Information
PC-63515

BI8626

1875036-75-1

BI8626 (BI-8626) is a specific, small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 0.9 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b, IC50>50 uM); suppresses colony formation of Ls174T cells with IC50 of 0.7 uM; inhibits MYC-dependent transactivation in colorectal cancer cells, but not in stem and normal colon epithelial cells; stabilizes MYC-associated protein MIZ1.

PC-63514

BI8622

1875036-74-0

BI8622 (BI-8622) is a specific small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 3.1 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b); abolishes ubiquitination of MCL1 induced by ectopically expressed HUWE1 in HeLa cells with IC50 of 6.8 uM, suppresses colony formation of Ls174T cells with IC50 of 8.4 uM; inhibits MYC-dependent transactivation in colorectal cancer cells, but not in stem and normal colon epithelial cells; stabilizes MYC-associated protein MIZ1.

PC-62313

Tasisulam

519055-62-0

Tasisulam (LY 573636) is a small molecule antitumor agent that induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death; shows antiproliferative effect against a variety of human hematopoietic malignancies, including AML, B-ALL, large B-cell and mantle cell lymphoma cell lines; promotes the recruitment of RBM39 to the CUL4-DCAF15 E3 ubiquitin ligase, leading to RBM39 polyubiquitination and proteasomal degradation; causes aberrant pre-mRNA splicing.

Blood Cancer

Phase 1 Discontinued

PC-62312

Tasisulam sodium

519055-63-1

Tasisulam (LY 573636) is a small molecule antitumor agent that induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death; shows antiproliferative effect against a variety of human hematopoietic malignancies, including AML, B-ALL, large B-cell and mantle cell lymphoma cell lines; promotes the recruitment of RBM39 to the CUL4-DCAF15 E3 ubiquitin ligase, leading to RBM39 polyubiquitination and proteasomal degradation; causes aberrant pre-mRNA splicing.

Blood Cancer

Phase 1 Discontinued

PC-60879

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.

Solid Tumors

Phase 1 Clinical

PC-46931

Suramin sodium salt

129-46-4

Suramin sodium salt (BAY-205, NF-060) is an antitrypansomal drug that also possesses antitumor activity; inhibits CRL (Cullin-RING E3 ubiquitin ligases) activity by disrupting its ability to recruit Cdc34; induces accumulation of CRL substrates; also inhibits multiple viruses (ZIKVs, EV71).

Parasite Infection

Approved

PC-35959

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.

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