loop

Azosemide is a potent NKCC1 inhibitor (IC50s: 0.246 µM and 0.197 µM for hNKCC1A and NKCC1B).

Irigenin mediates its antimetastatic effect by specifically and selectively blocking the α9β1 and α4β1 integrin binding sites on the C-C loop of the Extra Domain A domain. It can sensitize TRAIL-induced apoptosis by enhancing the expression of pro-apoptotic molecules in gastric cancer cells and has anti-cancer effects.

Gap19 is a peptide that corresponds to a sequence on the cytoplasmic loop (CL) of Cx43.

YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13.

GroES mobile loop is a flexible region of unbound GroES that interacts with GroEL via the residues located at the tip of the loop.

D-loop peptide, synthetic is an antigenic peptide. It cyclizes through a peptide bond between the side chain carboxylic group of Asp10 and the terminal amide of the peptide.

Looplure is a chemosterilant, insect attractant and repellent.

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin.

Avapritinib (BLU-285) is a selective, highly potent, and orally active inhibitor of KIT and PDGFRA activation loop mutant kinases, targeting KIT D816V (IC50:0.27 nM) and PDGFRA D842V (IC50:0.24 nM), and attenuates the transport functions of ABCB1 and ABCG2. It binds to the active conformation of the kinases and exhibits antitumor activity.

FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/β-catenin signaling pathway.

Bumetanide (PF 1593) is a potent sulfamoylanthranilic acid derivative belonging to the class of loop diuretics. In the brain, bumetanide may prevent seizures in neonates by blocking the bumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC1), thereby inhibiting chloride uptake thus, decreasing the internal chloride concentration in neurons and may block the excitatory effect of GABA in neonates.

Trichlormethiazide (Naqua) is a short-acting, 3-dichloromethyl derivative of hydrochlorothiazide, belonging to the class of thiazide diuretics. Trichlormethiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule.

Torsemide (AC-4464) is an anilinopyridine sulfonylurea belonging to the class of loop diuretics. Torsemide has a prolonged duration of action compared to other loop diuretics, is extensively protein bound in plasma and has a relatively long half-life.

Ethacrynic acid (Edecrin) is a nonsulfonamide loop diuretic that inhibits the activity of the Na+/K+/2Cl- cotransporter NKCC2 in the thick ascending limb of the loop of Henle. It also inhibits glutathione S-transferase and Wnt signalling, producing cytotoxicity in chronic lymphocytic leukaemia cells and other tumour cells.

SR-29065 is a selective REV-ERBα agonist that inhibits BMAL1 transcription within the circadian transcription–translation feedback loop, and it has been applied to evaluate whether targeting both negative regulatory limbs of circadian control yields synergistic anti-tumor effects in glioblastoma models, supporting its broader use in autoimmune disorder and circadian rhythm research.

TLR1 is a cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic and inhibits IL-1 receptor-mediated responses.

C-MYC PEPTIDE EPITOPE TFA, the product of the c-myc proto-oncogene, is a helix-loop-helix leucine zipper phosphoprotein that regulates gene transcription in cell proliferation, cell differentiation and apoptosis. This peptide is a human c-myc epitope.

Zatebradine hydrochloride (UL-FS-49CL) is a highly effective and effective HCN Channel inhibitor (IC50:1.96 µM). HCN Channel is an effective hyperpolarization activated loop nucleotide gated channel. Zatebradine hydrochloride blocks slow inward currents through human HCN1, HCN2, HCN3, and HCN4 channels with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM, and 1.88 µM, respectively.

PDdB-Pfp is a reducible ADC (antibody-drug conjugate) linker designed for agents targeting the extracellular loop 1 (ECL1) of TM4SF1 (transmembrane 4 L6 family member 1).

PDP-Pfp is a reducible ADC linker primarily used for targeting agents directed at the extracellular loop 1 (ECL1) of TM4SF1, a member of the transmembrane 4 L6 family [1].

5,6-Dihydrouridine, a modified base, is located in conserved positions within the D-loop of tRNA in Eukaryota, Bacteria, and some Archaea.

Piretanide, an orally active loop diuretic, is recognized as a relatively safe and effective pharmacological agent with notable diuretic capacity. Piretanide exhibits potential for research in the treatment of congestive heart failure, with a distinct advantage due to its potassium-sparing properties that may reduce electrolyte imbalance. Piretanide can also be applied within experimental frameworks directed at the study of hypertension, further supporting its utility in cardiovascular research models.

DPQ is an antiviral compound. DPQ has also been shown to bind to a widened RNA major groove at the internal loop. DPQ acts against the H1N1 and H3N2 strains of influenza A as well as influenza B.

FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanisms in hepatocellular carcinoma cells. This leads to T-loop defects, inducing telomere shortening and cellular senescence. Additionally, FKB04 inhibits tumor growth in a human liver cancer xenograft mouse model (by implanting Huh-7 cells in BALB/c mice). This compound is utilized in research focused on liver cancer.