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.

FAP targeting peptide for FXX489 is the peptide component of FXX489. FXX489 is a targeting ligand that can specifically recognize and bind to fibroblast activation protein (FAP).

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.

dTAG Targeting Ligand 1 (SUBSTITUTE SHEET 245) serves as a ligand for target proteins in PROTAC (Proteolysis Targeting Chimera) applications. It is used in the synthesis of PROTACs.

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.

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.

FRα-targeting peptide C7 is a selective peptide ligand for folate receptor α (FRα), exhibiting specific binding capabilities to cells expressing FRα and potential for in vivo tumor targeting. This peptide is utilized in research for tumor diagnosis and therapy.

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

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.

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

Dupilumab (REGN-668) is a fully human monoclonal antibody targeting the alpha subunit of the interleukin-4 receptor, thereby inhibiting IL-4 and IL-13 signaling. As a systemic immunomodulator, it has demonstrated efficacy in improving atopic dermatitis.

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3 1 1 4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.

Trastuzumab deruxtecan (T-DXd) is an antibody-active molecule conjugate (ADC) with anticancer and antitumor activity, which is composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2) coupled to a topoisomerase I inhibitor (DXd). Trastuzumab deruxtecan has an improved effect on the treatment of HER2-positive breast cancer and gastric cancer.

AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells. [2]

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.

Z-VAD(OMe)-FMK is a pan-caspase inhibitor with irreversible properties; Z-VAD(OMe)-FMK is also an inhibitor of ubiquitin C terminal hydrolase L1 (UCHL1), which is irreversibly modified by targeting the UCHL1 active site.

Go 6983 is a PKC inhibitor with IC50 values of 7, 7, 6, 10, and 60 nM for PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, respectively. Go 6983 has antitumor activity, cardiovascular protection, and protein kinase C inhibition.