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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-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-35676

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.
PC-35675

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.

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