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cIAP1 E3 ligase inhibitor D19

Chemical Structure : cIAP1 E3 ligase inhibitor D19

CAS No.: 380640-76-6

cIAP1 E3 ligase inhibitor D19 (cIAP1 inhibitor D19)

Catalog No.: PC-35675Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 325.404
Formula C16H11N3OS2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-2-((2-(benzo[d]thiazol-2-yl)hydrazono)methyl)benzo[b]thiophen-3-ol

References

1. Li H, et al. Proc Natl Acad Sci U S A. 2018 Sep 4. pii: 201807711.

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