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.

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.

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.

Looplure is a chemosterilant, insect attractant and repellent.

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation, with IC₅₀ values of 5 µM and 8 µM, respectively. D-I03 exerts significant growth inhibition on BRCA1/2-deficient cancer cells but has no effect on RAD51. D-I03 can be used in combination therapy studies for tumors with DNA damage repair defects.

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.

TH9028 is an inhibitor targeting MTHFD1, MTHFD2, and MTHFD2L, with IC50 values against the human-derived targets of 0.5 nM (MTHFD1), 11 nM (MTHFD2), and 27 nM (MTHFD2L), respectively. This compound binds to the substrate-binding region of the target enzymes, forming hydrogen bonds and other interactions with key amino acid residues, while also inducing conformational changes in the loop 1 region of the enzyme. Functionally, TH9028 slows down the progression of replication forks, induces replication stress, causes cell cycle arrest at the S phase, promotes apoptosis, inhibits thymidine synthesis, and leads to the misincorporation of uracil into DNA. In acute myeloid leukemia and T-ALL cells, TH9028 exhibits antiproliferative activity, while its effects on non-transformed cells are relatively weak. Therefore, TH9028 can be used in research related to acute myeloid leukemia.

AP23464 represents a highly specialized ATP-based small molecule tyrosine kinase inhibitor specifically engineered to target the catalytic domain of Abl and Src kinases along with the Kit receptor with exceptional inhibitory potency and selectivity, effectively facilitating the measurable blockade of phosphorylation-mediated signaling across various preclinical experimental models to evaluate the suppression of oncogenic driver activities during strictly monitored laboratory observation periods and biochemical investigations to ensure high experimental sensitivity.

CGP74514A is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor with an IC50 of 25 nM. It effectively inhibits the activity of the CDK1/cyclin B complex, arrests the cell cycle at G2/M phase, and further induces apoptosis in tumor cells, showing promising application prospects in bladder cancer research.

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.