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Cat. No. Product Name CAS No. Information
PC-35913

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.

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-61253

DT204

428497-71-6

DT204 (DT-204) is a novel SCFSkp2 inhibitor that reduces Skp2 binding to Cullin-1 and Commd1, synergistically enhances BTZ-induced apoptosis; stablizes and increases p27 levels, does not increase the level of p53, demonstrates potential synergy with CI values of 0.7, 0.8 and 0.7 for RPMI8226, U266 and MM1.S respectively combined with 1 nM BTZ, co-treatment induces apoptosis in cells resistant to the proteasome inhibitors BTZ, carfilzomib or ixazomib; overcomes drug resistance and reduces the in vivo growth of myeloma tumors in murine models.

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

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