site-specific

Itaconate-alkyne (ITalk) is a bioorthogonal probe for quantitative, site-specific chemoproteomic profiling of itaconate in inflammatory macrophages, facilitating biochemical evaluation and proteomic analysis of its direct targets.

CGP 78608 hydrochloride is a specific antagonist at the glycine binding site of the NMDA receptor (IC50 = 6 nM). CGP 78608 hydrochloride exhibits anticonvulsant activity. CGP 78608 hydrochloride potentiates GluN1/GluN3A-mediated glycine currents (estimated EC50 = 26.3 nM).

A 21960 (Ethyl 2-chloroacetoacetate) inhibits synapse formation between resolvase and two directly repeated res sites, blocks site-specific recombination reactions, and can be used to study bacterial infections.

Rac1 Inhibitor W56 acetate(1095179-01-3 free base) is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 acetate(1095179-01-3 free base) selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

Unesbulin (PTC596) is an orally active, selective inhibitor of B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1).

Bis-PEG4-NHS ester is a bis-N-hydroxysuccinimide-activated tetraethylene glycol crosslinker. Bis-PEG4-NHS‘s NHS groups selectively condense with primary amines to form stable amide bonds, thereby covalently crosslinking proteins, peptides, or small molecules. The PEG4 moiety in Bis-PEG4-NHS ester confers good water solubility and flexibility to the conjugate, effectively suppresses nonspecific adsorption, and reduces steric hindrance, thereby supporting site-specific, copper-free click chemistry coupling between antibodies and liposomes. Bis-PEG4-NHS ester can be used for the preparation of homogeneous antibody-drug conjugates (ADCs) and the modular construction of PROTAC bifunctional molecules.

Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs) for the preparation of neolymphostin-based ADC precursors, specifically for site-specific cysteine mutant trastuzumab-A114C conjugation[1].

PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. PKR-IN-C16 protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.

(2-Pyridyldithio)-PEG4 acid is a four-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. It serves as a crucial component in the conjugation of antibodies and drugs, enabling targeted drug delivery and enhanced therapeutic efficacy. This linker possesses a (2-pyridyldithio) group at one end, facilitating the attachment of the linker to the specific site on the antibody molecule. The PEG4 chain provides the necessary flexibility and biocompatibility for optimal drug release while maintaining stability throughout the circulation in the body. Ultimately, (2-Pyridyldithio)-PEG4 acid is instrumental in the development and advancement of ADCs, a promising approach in cancer therapy.

Boc-D-2,3-diaminopropionic acid (N-t-Boc-amino-D-alanine) is a derivative of an amino acid featuring a Boc protecting group. It is utilized in the synthesis of a powerful NMDA receptor glycine site agonist that exhibits specific activity towards the GluN2 subunit.

PV1162 is a Chk2-specific inhibitor characterized by a potency with an IC 50 value of 0.29 nM. It operates by specifically targeting the gatekeeper-dependent hydrophobic pocket behind the ATP-binding site (adenine-binding region) to inhibit ATP binding to Chk2, effectively suppressing the phosphorylation activity of Chk2. This compound has demonstrated potential for application in cancer therapy.

NeoSTX (Neosaxitoxin) is a specific sodium channel blocker that targets site 1. It works synergistically with local anesthetics to provide surgical anesthesia through peripheral nerve block or local infiltration and significantly prolongs postoperative analgesia duration.

Diglycyl-histidine is a tripeptide complexed with cupric ion designed to mimic specific Cu(II) transport site of ascorbate on albumin molecule.

MS8511 hydrochloride is a selective G9a/GLP inhibitor with IC50 values of 100 nM and 140 nM respectively, exhibiting covalent and irreversible characteristics. MS8511 reduces intracellular H3K9me2 levels and enhances anti-proliferative activity, making it suitable for investigating multiple cancers.

Metaphit methylsulfate is a specific PCP antagonist and an acylating agent for the [3H] phencyclidine binding site in rat brain homogenate. It inhibits PCP-induced motor activity through a presynaptic mechanism.

5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione is a Thalidomide analog featuring a hydroxyl group, which serves as a versatile site for further derivatization. Thalidomide acts as an E3 ligase activator and facilitates the ubiquitination of specific proteins.

ZK-806450 is a compound with antiviral properties. It exhibits high binding potential to the allosteric site of the SARS-CoV-2 3CL protease and is capable of specific and stable interaction with the GAG site of the dengue virus envelope protein.

Transthyretin-IN-3 (compound 6) is a synthetically designed benzofuran analogue. It selectively binds with transthyretin in plasma, inhibiting amyloid aggregation with an IC50 of 5.0±0.2 μM. By incorporating a chlorine substituent at a specific position, Transthyretin-IN-3 effectively targets the thyroxine binding site of TTR, preventing the dissociation of TTR tetramers into unstable monomers.

Antiparasitic agent-32 (compound M9) is an analogue of Piperaquine and acts as a potent antiparasitic agent targeting plasmodium falciparum lactate dehydrogenase (Pf LDH) with a Pf3D7IC50 of 0.40 μM. It demonstrates significant activity against both the asexual and gametocyte stages of plasmodium falciparum. Its antimalarial effect is achieved through stable and specific non-covalent interactions at the NADH binding site. Antiparasitic agent-32 is applicable in malaria research.

4A-BFA-11 is a folate-targeted PEG-MMAE conjugate with specific binding affinity for the folate receptor α (FR-α) (KD= 106.7 nM). It achieves tumor accumulation by combining PEG-mediated long circulation (EPR effect) with folate receptor targeting. At the tumor site, 4A-BFA-11 undergoes enzymatic cleavage to release the active payload, ensuring precise action. In HeLa mouse models, 4A-BFA-11 effectively delivers, targets, and regulates the release of MMAE within tumor tissues. This compound can be applied in research involving cervical cancer, ovarian cancer, and lung cancer.

VU 0285683 is a specific negative allosteric modulator of mGluR5 with a high affinity for the MPEP binding site. VU 0285683 shows anxiolytic-like activity.

A-20832 inhibits resolvase-promoted site-specific recombination postsynaptically at strand cleavage. It does not inhibit resolvase binding to res, as measured by filter binding, or synapse formation. DNase I analysis in the presence of A-20832 indicates t

Coralyne chloride is a protoberberine with strong anticancer activity. It can be used to prepare Coralyne derivatives, a fluorescent DNA-based molecular rectifier built into DNA duplexes through site-specific insertion. It acts as a topoisomerase I toxic molecule, inducing topoisomerase I-mediated DNA cleavage.

1-Amino-1-deoxy-D-fructose is an amino monosaccharide.1It induces site-specific DNA damage at pyrimidine residues in cell-free assays. 1-Amino-1-deoxy-D-fructose moieties have been found as a component of fructosamines, glycated serum proteins that are elevated in patients with conditions such as diabetes.2,3