T21793

CGP 35348 is a selective antagonist of GABAB receptor (EC50 = 34 μM). CGP 35348 can be used in studies of neuromuscular coordination and spatial learning after neonatal brain damage in albino mice.

Fmoc-Gly-Gly-Phe-Gly-Paclitaxel (Compound 16a-3) is a drug-linker conjugate utilized in ADCs (antibody-drug conjugates). It incorporates the ADC linker Fmoc-Gly-Gly-Phe-OH along with the potent microtubule polymerization inhibitor, Paclitaxel. This compound is applicable in cancer research.

GCB-27b is an immune stimulant that binds to CD1d. It forms a stable and long-lasting complex with CD1d, which is presented to TCRs on NKT cells to drive immune responses. In *Mus musculus* (house mouse), GCB-27b induces a Th1-biased immune response, resulting in high IFN-γ expression while restricting IL-4 levels. GCB-27b is suitable for research related to melanoma lung metastasis.

GPR84 antagonist10 (compound 1) is a potent and orally active GPR84 antagonist. It is suitable for investigating GPR84-dependent conditions, such as inflammation-driven pain disorders.

WWZ-11-098 is a selective CDK6 degrader with a DC50 of 2.6 nM. It induces CDK6 degradation in a CRBN-dependent manner without affecting CDK1, CDK2, CDK4, or CDK9. WWZ-11-098 triggers apoptosis, causes G1-S cell cycle arrest, and exhibits antiproliferative activity in cancer cells. In xenograft models, it demonstrates antitumor efficacy without signs of toxicity. This compound is applicable for leukemia research.

DPP-1-IN-2 is a potent DPP-I inhibitor with a human IC50 of 36.8 nM and demonstrates oral efficacy. It binds to DPP-I within cells, enhancing its thermal stability and inhibiting its enzymatic activity, thereby reducing the activity and expression levels of downstream neutrophil serine proteases. Additionally, DPP-1-IN-2 modulates the secretion of inflammatory cytokines and chemokines, exerting anti-inflammatory effects. It can reverse joint inflammation and tissue damage in an adjuvant-induced arthritis rat model and is applicable for research related to arthritis.

FAPI-X5 is an inhibitor of fibroblast activation protein (FAP). It binds to the catalytic domain of FAP, forming hydrogen bonds and engaging in π-π stacking with key active residues, resulting in functional inhibition. FAPI-X5 exhibits albumin-binding activity, which extends its systemic circulation half-life. It shows cytostatic effects on glioblastoma cells, slowing tumor growth without causing tumor regression. When labeled with [^68Ga], FAPI-X5 serves as a PET tracer, displaying rapid tumor uptake and high-contrast imaging in glioblastoma-bearing mice. Additionally, when labeled with [^177Lu] or [^47Sc], it acts as a targeted radionuclide therapeutic, offering prolonged tumor retention. FAPI-X5 is applicable in glioblastoma research.

1,3-Bis-aminooxy propane dihydrochloride is a PROTA Clinker that belongs to the alkyl chain category and can be used in the synthesis of PROTAC molecules.

FWG-33B is an activator of the TRMT112:METTL5 complex, with an IC50 value of 0.47 μM. It is applicable for research related to breast cancer, hepatocellular carcinoma, and nasopharyngeal carcinoma.

DNA Gyrase/ribosomes-IN-1 is an inhibitor of bacterial ribosomes (ribosome) and DNA gyrase (DNA gyrase), with IC50 values of 1.11 μM and 3.31 μM, respectively. It also inhibits CYP3A4 with an IC50 of 18.5 μM and demonstrates stability in mouse plasma and liver microsomes. By interacting with ribosomal RNA and associated sites, DNA Gyrase/ribosomes-IN-1 can inhibit bacterial protein synthesis, and by interacting with the gyrase complex, it hinders bacterial DNA replication. It can restore activity against macrolide-resistant Gram-positive pathogens mediated by erm and enhances activity against Gram-negative bacteria such as Haemophilus influenzae (H. influenzae) and Moraxella catarrhalis (M. catarrhalis). DNA Gyrase/ribosomes-IN-1 is applicable for the study of community-acquired bacterial pneumonia.

PROTAC SARS-CoV-2 Mpro degrader-7 is a PROTAC degrader targeting the SARS-CoV-2 main protease (Mpro), with a DC50 of 0.985 μM. It facilitates K48-linked poly-ubiquitination of SARS-CoV-2 Mpro, leading to proteasome-dependent degradation via the ubiquitin-proteasome system. The compound forms a ternary complex with SARS-CoV-2 Mpro and CRBN E3 ubiquitin ligase, enabling ubiquitination of the viral protease. It has a high selectivity index and induces dose-dependent degradation of SARS-CoV-2 Mpro in cell lines expressing the viral protease. PROTAC SARS-CoV-2 Mpro degrader-7 is applicable in studies related to COVID-19.