CFTR

PTC124 also known as Ataluren is CFTR-G542X nonsense allele inhibitor.

CFTRinh-172 is a voltage-independent, selective CFTR inhibitor

CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 uM).

Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy.

Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders.

Glafenine is a non-selective, non-steroidal anti-inflammatory drug (NSAID) that inhibits both COX-1 and COX-2 enzymes. It exerts anti-inflammatory, anti-proliferative, and anti-migratory effects by suppressing the arachidonic acid metabolic pathway, thereby reducing prostaglandin production. Additionally, glafenine induces cell cycle arrest in vascular smooth muscle cells and endothelial cells and decreases the synthesis of the extracellular matrix protein tenascin. It is utilized in research related to inflammatory disorders, vascular restenosis, and cystic fibrosis.

BPO-27 racemate is a potent cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor, exhibiting an IC50 of 8 nM. This compound has been shown to effectively suppress CFTR activity, making it valuable for research aimed at understanding CFTR-related disorders. BPO-27 racemate can be utilized in studies investigating ion channel regulation and potential therapeutic interventions for cystic fibrosis.

PPQ-102 is a compound that targets intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR- mediated chloride current in a voltage-dependent and reversible manner.

IOWH032 is a CFTR inhibitor.

(R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM.

PGD97 is a selective cyclic peptide inhibitor that targets the CAL/CFTR interactions, exhibiting a KD value of 6 nM for its desulfide cyclized form at the CAL PDZ domain. Demonstrating a selectivity of ≥ 130-fold compared to NHERF1/2 PDZ domains, PGD97 effectively stabilizes F508del-CFTR at the cell membrane, enhancing CFTR function essential for maintaining fluid homeostasis in the lung. This compound is valuable for research applications focused on cystic fibrosis.

Steviol is a selective inhibitor of the aquaporin-2 (AQP2) and cystic fibrosis transmembrane conductance regulator (CFTR) proteins. This compound impedes renal cyst growth by inhibiting CFTR activity, which leads to decreased AQP2 expression and promotes the degradation of both AQP2 and CFTR. Steviol is relevant for research focused on polycystic kidney disease and mechanisms underlying renal cyst development.