DC-LC3in-D5 is a potent, selective covalent inhibitor of LC3A/B that disrupts autophagy by targeting Lys49 on LC3B, a key residue in the LC3-interacting region (LIR) interface. It inhibits the LC3B-LBP2 interaction with an IC₅₀ of 200 nM and exhibits a K_inact/K_i of 0.36 μM⁻¹·min⁻¹, indicating efficient covalent binding . In HeLa cells, treatment with DC-LC3in-D5 at concentrations of 3–30 μM for 16 hours leads to impaired LC3B lipidation, accumulation of the autophagy substrate p62, and a significant reduction in autophagosome formation . Activity-based protein profiling confirms its high selectivity for LC3A/B, with minimal off-target interactions across the proteome . Importantly, DC-LC3in-D5 exhibits low cytotoxicity, with GI₅₀ values exceeding 100 μM in various human cell lines, making it a valuable tool for autophagy research and potential therapeutic applications
MedKoo Cat#: 556389
Name: DC-LC3in-D5
CAS#: 2868312-73-4 (free base)
Chemical Formula: C19H22Cl2N2O3
Exact Mass: 396.1007
Molecular Weight: 397.30
Elemental Analysis: C, 57.44; H, 5.58; Cl, 17.85; N, 7.05; O, 12.08
The following data is based on the product molecular weight 397.30 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
