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Heclin | HECT domain containing E3 ubiquitin ligase inhibitor

Heclin (890605-54-6) is the first small molecule inhibitor of the HECT domain-containing E3 ubiquitin ligases. Heclin (HECT ligase inhibitor) inhibits several HECT ligases in cultured cells, IC50s = 6.8, 6.3 and 6.9 μM for Smurf2, Nedd4 and WWP1 respectively. It does not block E2 binding but causes a conformational change which results in oxidation of the active site cysteine. Cells tolerate heclin treatment for several hours but exposure for 24 hours leads to death in HEK293 cells, consistent with an essential role for HECT ligase activity in mammalian cells. Heclin does not inhibit RING domain ligases. Thus it is a valuable tool for distinguishing between RING and HECT-mediated ubiquitination1.

References/Citations
1) Mund et al. (2014), Peptide and small molecule inhibitors of HECT-type ubiquitin ligases; Proc. Natl. Acad. Sci. USA, 111 16736

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Catalog#  10-1534

$60.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
890605-54-6
Activity:
HECT domain containing E3 ubiquitin ligase inhibitor
Chemical Name:
2E-N-(4-Acetylphenyl)-3-(5-ethylfuran-2-yl)prop-2-enamide
Molecular Weight:
283.33
Molecular Formula:
C17H17NO3
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 10 mg/ml).
Physical Properties:
Beige solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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