targets

Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.

Procaine hydrochloride (Novocaine HCl) is the hydrochloride salt form of procaine, a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodiumchannels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. In addition, this agent increases electrical excitation threshold, reduces rate of rise of action potential and slows nerve impulse propagation thereby causing loss of sensation.

Datopotamab deruxtecan (DS-1062) is an antibody-drug conjugate (ADC) that targets tropomyosin 2 (TROP2) on the surface of trophoblast cells. Datopotamab deruxtecan exhibits antitumor activity by specifically binding to TROP2 and internalizing, releasing DXd to inhibit topoisomerase I (IC₅₀ = 0.31 μM), thereby inducing DNA damage and apoptosis. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

Ponsegromab (PF 06946860) is a selective and potent humanized anti-GDF15 antibody inhibitor with IC₅₀ values of 0.123 nM, 0.053 nM, and 0.102 nM for human, rhesus macaque, and mouse targets, respectively. Ponsegromab exhibits anti-cachexia activity by binding to GDF15 to prevent its interaction with GFRAL, thereby disrupting GDF15/GFRAL-mediated signaling. Ponsegromab possesses potential anticancer activity and may be used to treat cancer patients with cancer anorexia-cachexia syndrome. Ponsegromab acts as a chemopreparative agent, increasing intracellular reactive oxygen species levels and reducing glutathione levels.

Adalimumab (anti-TNF-alpha) is the first fully human recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha.

Zolbetuximab(IMAB362) is a monoclonal antibody that specifically targets Claudin-18.2.Zolbetuximab has potential antitumor activity, mediating killing of Claudin-18.2-positive cells through an immune effector mechanism.Zolbetuximab is used in the study of gastrointestinal adenocarcinomas and pancreatic tumors.

Atezolizumab is an antibody inhibitor, a humanized monoclonal antibody, IgG1, which targets PD-L1 and blocks the interaction of PD-L1 with PD-1. Atezolizumab has antitumor activity and promotes T-cells to attack tumor cells.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Mitoquinone mesylate (MitoQ10 mesylate) is a potent TRAP1 inhibitor (IC50=0.2 μM). Mitoquinone mesylate is an antioxidant that prevents oxidative damage and targets mitochondria of TPP.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

SQ109 (NSC 722041) is an ethambutol (EMB) derivative and a specific inhibitor of MmpL3, exhibiting potent anti-Mycobacterium tuberculosis activity. SQ109 effectively inhibits the adult stage of the parasite Trypanosoma and kills cells, with an IC50 of 50 ± 8 nM. SQ109 can be used in tuberculosis and antiparasitic research.

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) delivering a topoisomerase I (TopoI) inhibitor that targets EGFR and c-MET, inducing DNA double-strand breaks and inhibiting the growth of non-small cell lung cancer cells.

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]

dTAGV-1 TFA is a highly efficient, highly selective VHL-dependent PROTAC-mediated protein degrader that specifically targets and degrades mutant FKBP12 fusion proteins. dTAGV-1 TFA efficiently induces the degradation of FKBP12 fusion proteins at both the cellular and in vivo levels.

V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively targets the amino acid transporter ASCT2 (SLC1A5) without affecting ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake in HEK-293 cells (IC50=9.6 μM). V-9302 can be used for research on tumor and amino acid transport

KDM4-IN-4 is a histone lysine demethylase 4 (KDM4) inhibitor that primarily targets the Tudor domain of KDM4A and exhibits anticancer activity. KDM4-IN-4 has an affinity for the KDM4A Tudor domain of approximately 80 μM. KDM4-IN-4 inhibits the binding of H3K4Me3 to the Tudor domain in cells, with an EC50 of 105 μM. KDM4-IN-4 can be used in cancer research.

Cyclo(-RGDfK) is a potent and selective inhibitor of integrin αvβ3 with IC50 of 0.94 nM. Cyclo specifically targets tumor microvasculature and cancer cells by binding to αvβ3 integrin on the cell surface.

Cadonilimab (AK104) is a tetravalent PD-1/CTLA-4 bispecific humanised antibody that activates T cells by enhancing IL-2 and IFN-γ secretion while reducing pro-inflammatory cytokine secretion (e.g., IL-6, IL-8). It offers low toxicity and high affinity, making it suitable for metastatic cervical, gastric, hepatic, and pulmonary cancers, pancreatic cancer, and oesophageal squamous cell carcinoma.

Tarlatamab (AMG-757) is a bispecific T cell engager (BiTE) antibody targeting DLL3 and CD3, with human DLL3 and CD3 KD = 0.64 nM/14.9 nM, for use in immuno-oncology therapy of small cell lung cancer (SCLC).

Aducanumab (BIIB037), A selective human immunoglobulin gamma-1 (IgG1) monoclonal antibody, targets the clustered form of amyloid beta (Aβ). Aducanumab shows brain permeability and may be used to treat Alzheimer's disease (AD).

Anti-Mouse Ly6G Antibody (1A8) is an anti-mouse Ly6G antibody that binds to Ly-6G on neutrophils and can be used for flow cytometry analysis and studies of neutrophil infiltration, recruitment and migration.

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. Using β-NF as an AhR ligand, it targets bromodomain (BRD)-containing proteins and induces AhR and BRD protein interactions. β-NF-JQ1 exhibits potent anticancer activity associated with protein knockdown activity.