| Bioactivity | KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family[1]. |
| Target | IC50: 3.5 μM (a active site of PDIA1), 104.5 μM (a′ active site of PDIA1) |
| Invitro | KSC-34 is selective for PDIA1 over other members of the PDI family, and other cellular cysteine-containing proteins. KSC-34 contains a (4-phenylbutyl)methylamine diversity element for optimized binding to the active site of the a domain of PDIA1 with a chloroacetamide electrophile for covalent modification of C53 on PDIA1[1]. |
| Name | KSC-34 |
| CAS | 2226201-97-2 |
| Formula | C21H28ClN7O |
| Molar Mass | 429.95 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. Cole KS, et al. Characterization of an A-Site Selective Protein Disulfide Isomerase A1 Inhibitor. Biochemistry. 2018;57(13):2035-2043. |