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VA-K-14 hydrochloride(VAK14 HCl) is a selective thyrotropin receptor (TSHR) antagonist (IC50= 12.3 μM) that inhibits TSHR stimulation by serum and monoclonal TSHR-stimulating antibodies from patients with GD and abrogates TSHR signaling.

Z-VA-DL-D-FMK (Z-VA-DL-D(OH)-FMK) acts as an inhibitor of caspases. It irreversibly binds to caspases, enhancing the sensitivity to TNF-α and stimulating HIV replication in infected T cells ACH-2.

BCN-HS-PEG2-VA-PABC-SG3199 (Compound 4) functions as a pyrrolobenzodiazepine-based agent linker for antibody-drug conjugates (ADC) [1]. This compound also serves as a click chemistry reagent, featuring a BCN group capable of participating in strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules.

DBCO-PEG4-VA-PBD is a cleavable 4-unit PEG ADC linker utilized in antibody-drug conjugate (ADC) synthesis [1].

VA-111913, a vasopressin receptor antagonist, is used potentially for the treatment of dysmenorrhea.

MC-VA-T-moiety(CH2-NH-CH3)–Exatecan (compound 11-5) serves as a Drug-Linker Conjugate for ADC, capable of synthesizing ADCs that exhibit anticancer activity [1].

Fmoc-VA-PAB-PNP is a cleavable linker with an Fmoc protecting group, which can be used in the synthesis of ADCs.

MC-VA-PAB-PNP is a cleavable ADC linker that can be used for the synthesis of antibody-conjugated active molecules (ADCs).

Mal-PEG4-VA, a noncleavable ADC linker featuring a Maleimide group, is utilized in the synthesis of antibody-drug conjugates.

MC-VA-PAB-Exatecan is an agent-linker conjugate designed for Antibody-Drug Conjugate (ADC) applications, comprising the ADC linker (peptide MC-VA-PAB) and the DNA topoisomerase I inhibitor Exatecan. Synthesis of this conjugate has demonstrated promising antitumor activity [1].

Aristolochic acid Va, a natural compound, is isolated from Aristolochia plants [1].

MC-VA-PAB-MMAD is a thiol-reactive Drug-linker. MMAD is an effective microtubule (tubulin) inhibitor, which is commonly used in the synthesis of antibody-drug conjugates (ADCs).

MC-VA-PABC-MMAE is a conjugate composed of the ADC linker peptide MC-VA-PABC and the cytotoxic agent monomethyl auristatin E (MMAE), a potent inhibitor of tubulin polymerization [1] [2]. It functions as an agent-linker module for antibody-drug conjugates (ADCs).

Mal-va-mac-SN38 is a conjugate molecule functioning as an ADC (Antibody-Drug Conjugate) drug-linker. This compound comprises the cytotoxic ADC agent SN-38 and a linker. Once inside the body, Mal-va-mac-SN38 rapidly forms a covalent bond with endogenous albumin, resulting in the formation of HSA-va-mac-SN38. It demonstrates remarkable stability in human plasma and exhibits both antitumor and antimetastatic properties.

Mal-PEG4-VA-PBD is a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), consisting of the antitumor antibiotic Pyrrolobenzodiazepine (PBD) linked via Mal-PEG4-VA.

SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells. This compound undergoes in situ conversion to active PROTAC via a copper-catalyzed click reaction utilizing endogenous copper present in tumor tissues. Additionally, SA-VA induces apoptosis and arrests cell cycle progression in the S phase [1].

VA-PAB-DMEA-PNU159682 is a transpeptidase reaction-type Drug-linker with an innovative highly stable and degradable linker. PNU159682 is a DNA topoisomerase II (Topo II) inhibitor with excellent cytotoxicity and can be used in the synthesis of antibody-drug conjugates (ADCs).

Mal-PEG8-VA-PAB-PNP is a degradable, hydrophilic linker that can be used in the synthesis of ADCs.

Vadimezan (DMXAA) is a vascular disrupting agent, a murine STING agonist, and an inducer of cytokines such as type I IFN. Vadimezan has antitumor activity and induces a rapid cessation of blood flow in tumors without affecting blood flow in normal tissues.

ZINC40099027 is a specific adhesion plaque kinase (FAK) activator that promotes gastric mucosal repair in persistent aspirin-associated gastric injury through activation of adhesion plaque kinase, activates human adhesion plaque kinase by accelerating the enzyme activity of the structural domain of FAK kinase, activates cytosolic FAK, and promotes intestinal epithelial wound closure.

Z-VAD-FMK (Caspase Inhibitor VI) is a broad-spectrum inhibitor of caspases.Z-VAD-FMK binds to activated caspases and inhibits apoptosis.Z-VAD-FMK does not inhibit UCHL1 activity, even at concentrations up to 440 μM.

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.

NF-κΒ activator 1 can activate the nf-kappa Β gene activator, EC50 of 0.9 microns. NF-κΒ is widely used in eukaryotic cells as a gene regulating cell proliferation and cell survival. NF-κΒ activator 1 induces superoxide dismutase (SOD) 2 1 mRNA expression.

Bevacizumab, a humanized monoclonal antibody, specifically and with high affinity binds to all isoforms of VEGF-A.