Heclin, HECT E3 Ubiquitin Ligase Inhibitor

Heclin is a selective HECT E3 ubiquitin ligase inhibitor, inhibits Nedd4, Smurf2 and WWP1 with IC50 6.3, 6.8 and 6.9 μM respectively. It is selective for HECT-mediated over RING-mediated ubiquitination. Heclin does not block E2 binding but causes a conformational change that results in oxidation of the active site Cys. It kills HEK293 cells growing in culture, consistent with an essential role for HECT ligase activity in mammalian cells.

Product information

CAS Number: 890605-54-6

Molecular Weight: 283.32

Formula: C17H17NO3

Chemical Name: N-(4-Acetylphenyl)-3-(5-ethyl-2-furanyl)-2-propenamide

Smiles: CC(=O)C1C=CC(=CC=1)NC(=O)C=CC1=CC=C(CC)O1

InChiKey: SPTWXRJNCFIDRQ-ZHACJKMWSA-N

InChi: InChI=1S/C17H17NO3/c1-3-15-8-9-16(21-15)10-11-17(20)18-14-6-4-13(5-7-14)12(2)19/h4-11H,3H2,1-2H3,(H,18,20)/b11-10+

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Heclin was used at 10-30 µM final concentration in various in vitro assays.

References:

1. Mund T, et al. Peptide and small molecule inhibitors of HECT-type ubiquitin ligases. (2014) Proc Natl Acad Sci USA. 111(47):16736-41.

Products are for research use only. Not for human use.

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