KM11060

SKU: orb1224025

Description

A potent corrector of the F508del-CFTR trafficking defect that partially restores F508del trafficking and increases maturation significantly in BHK cells (10 nM for 24 h or 10 uM for 2 h); also can significantly increase plasma lipoxin A4 levels in F508del relevant to wildtype mice.

Key Properties

• CAS Number: 774549-97-2
• MW: 422.3282
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₇Cl₂N₃O₂S
• SMILES: O=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C23)CC1)(C4=CC=C(Cl)C=C4)=O
• Target: CFTR
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  In LPS-induced acute lung inflammation, blockade of PSGL-1 (P-selectin glycoprotein ligand-1) or P-selectin, antagonism of PAF by WEB2086, or correction of mutated CFTR trafficking by KM11060 could significantly increase plasma lipoxin A4 levels in F508del relevant to wildtype mice.
• In Vitro:
  Small-molecule correctors such as KM11060 may serve as useful pharmacological tools in studies of the F508del-CFTR processing defect and in the development of cystic fibrosis therapeutics. KM11060 rescues F508del-CFTR trafficking in cultured cells and native epithelial tissues. KM11060 partially corrects F508del-CFTR processing and increases surface expression to 75% of that observed in cells incubated at low temperature. Up to 50% of the F508del-CFTR in cells treated with KM11060 was complex-glycosylated, indicating passage through the Golgi. KM11060 as a promising compound for further development of CF therapeutics.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KM 11060 | KM-11060

Quick Database Links

Gene Symbol

CFTR