targeting

Itch-Targeting Compound 1 is an anti-itch agent effective in preventing or treating reactions from insect bites, environmental allergens, skin infections, external vermination, or itching in renal dialysis patients.

Neuromuscular-targeting compound 1 can be used to study muscular dystrophy and neuromuscular-related diseases.

Cancer-Targeting Compound 1 can be used in the study of hormone-related cancers, including the treatment or prevention of fibroids, uterine leiomyomas, polycystic ovarian syndrome, or hormone-dependent Cancer, among others.

Neuromuscular Disorder-Targeting Compound 1 is utilized in research for neuromuscular disorders, including chronic fatigue syndrome and fibromyalgia syndrome symptoms.

Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor [1].

Arrhythmias-Targeting Compound 1 is a compound. It is used in the research of arrhythmias.

Arrhythmic-Targeting Compound 1, used for arrhythmic disease, contains nitrogen-containing spirocycles.

Urinary Incontinence-Targeting Compound 1, used in the research of urinary incontinence, is a sulfonanilide derivative.

Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.

Dxd (OQM5SD32BQ) is a potent DNA topoisomerase I inhibitor (IC50= 0.31 μM). Dxd was used as a conjugate drug for HER2-targeted ADCs.

TSPO ligand-2 (Carbonic acid) is a ligand of AUTAC1 which contains a p-fluorobenzylguanine and a Fumagillol moiety.

TPP-1, a peptide inhibitor, targets the interaction between programmed cell death protein 1 (PD-1) and its ligand (PD-L1), binding specifically to PD-L1 with a dissociation constant (Kd) of 94.67 nM. At a concentration of 20 µM, TPP-1 effectively counteracts the PD-L1-induced suppression of IFN-γ production in anti-CD3-stimulated isolated human CD4+ T cells. Furthermore, TPP-1 demonstrates significant efficacy in reducing tumor volume in a mouse xenograft model of HL-60 leukemia. This model involved HL-60 cells co-cultured with anti-CD3-activated isolated human CD4+ T cells, with TPP-1 administration at a dosage of 4 mg/kg showing notable antitumor activity.

Soluble epoxide hydrolase (sEH) PROTAC 1a is a proteolysis-targeting chimera (PROTAC) comprising a cereblon ligand linked to the sEH inhibitor t-TUCB via a linker, promoting selective sEH degradation and inhibiting its hydrolase activity (IC50 = 0.8 nM) significantly more than its phosphatase activity (IC50 = >10,000 nM). This compound preferentially targets cytosolic sEH for lysosomal rather than proteasomal degradation. Furthermore, it mitigates thapsigargin-induced upregulation of phosphorylated inositol-requiring enzyme 1α (IRE1α) and X-box binding protein 1 (XBP1) splicing in HepG2 and 293T cells, thereby reducing endoplasmic reticulum stress.

G3BP1/2-Targeting ligand-1 is a ligand for G3BP1/2 and can be utilized as a targeting ligand in the synthesis of the G3BP1/2 PROTAC degrader PT-129.

FAP-targeting peptide-PEG2 conjugate (Example A1) is the polypeptide and linker conjugate component of Unlabeled FXX489. Unlabeled FXX489 serves as a ligand targeting fibroblast activation protein (FAP).

Peptide 46 is a short peptide that inhibits SC-dependent DNA synthesis by targeting the bacterial sliding clamp (SC).

(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor.

Breastcancertargeting peptide 18–4 is a keratin 1 (KRT1) receptor-targeting peptide with a dissociation constant (Kd) of 0.98 μM. Its amino acid sequence is WxEAAYQrFL, and it is an analogue of the P160 peptide. When covalently bonded with the anticancer peptide MccJ25, it significantly enhances MccJ25 uptake in breast cancer cells and boosts its anticancer efficacy. The IC50 values for this covalent compound are 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR, respectively.

FRα-targeting peptide C7 TFA is a selective peptide ligand for the folate receptor alpha (FRα) that specifically binds to FRα-expressing cells and has tumor-targeting capabilities in vivo. It is applicable in research related to tumor diagnosis and therapy.

GPC3 targeting peptide 1 TFA binds with GPC3, exhibiting a dissociation constant (Kd) of 0.23 nM.

Kidney-targeting peptide is a kidney-targeting peptide (KTP) that significantly enhances the renal targeting ability of Isoquercitrin. It is applicable to studies related to diabetic nephropathy.

Targeting thebacterialsliding clamp peptide 46 TFA is a short peptide that specifically targets the bacterial sliding clamp (SC) and inhibits SC-dependent DNA synthesis.

Herceptide (HER2-targeting peptide), a peptide that targets HER2, can be conjugated with the near-infrared fluorescent dye indocyanine green (ICG), facilitating the development of theranostic agents.

The FAP-targeting peptide for FXX489 constitutes the peptide moiety of FXX489, suitable for biochemical assays and drug synthesis studies. FXX489 is a fibroblast activation protein (FAP)-targeting ligand employed in radioligand therapy (RLT) for multiple cancers.