RAFKBP12 is a FKBP12 PROTAC degrader. RAFKBP12 demonstrates the feasibility of the CAP-TAC strategy, which enables proteasome-dependent degradation of FKBP12 that is independent of E3 ubiquitin ligases and protein ubiquitination. (Pink: FKBP12 ligand ; Blue: RPN13 ligand ; Black: linker).

RA190-PEG1-NH2, RA190 derivative, is an E3 ligase ligand. RA190-PEG1-NH2 can be used to synthesis FKBP12 PROTAC degrader RAFKBP12.

R214127 is a selective mGlu1 receptor antagonist with IC50 values of 6 and 14 nM for rat and human mGlu1a. R214127 acts on a site from the glutamate binding pocket, and competes for the same transmembrane segment VII as other noncompetitive mGlu1 antagonists.

R-130823 is an orally active, highly selective p38α inhibitor with an IC50 of 22 nM against p38α, an IC50 of 820 nM against p38β, and no activity against p38γ or p38δ. R-130823 downregulates downstream cartilage degradation and inflammatory mediators, and inhibits the release of MMP-13, MMP-1 and PGE2. R-130823 reduces hind paw swelling, improves hyperalgesia, and blocks arthritis progression.\nR-130823 is applicable to research related to osteoarthritis and rheumatoid arthritis.

R06039-696 is a neuropeptide S receptor (NPSR) agonist with an EC50 of 91 nM. R06039-696 can participate in regulating various biological functions such as arousal, stress and anxiety responses, memory processes, and food intake by activating NPSR.

R06039-636 is an agonist of the Neuropeptide S receptor (NPSR) with an EC50 value of 94nM.

Quinotolast is an orally active antiallergic agent. Quinotolast inhibits histamine release from rat peritoneal cells. Quinotolast inhibits cutaneous cromoglycate in guinea pig model. Quinotolast has inhibitory effect on histamine and peptide leukotrienes release from guinea pig lung fragments and mouse cultured mast cells. Quinotolast can be studied in allergy-related research.

Quindoxin is an antibacterial and growth promoter, commonly used in the livestock industry. Quindoxin exhibits clear dose-dependent mutagenic activity against Salmonella typhimurium TA98 and TA100 strains. Quindoxin can cause DNA damage and has potential genotoxicity and carcinogenic risks.

QS-IN-1 (Compound 10 in Table 2 on page 18) is a quorum sensing (QS) inhibitor with an IC50 of 1.22 μM against agr-type QS. QS-IN-1 is applicable to the research of bacterial infections.

PZ-1129 is a selective 5-HT7 receptor ligand with a Ki of 7 nM. PZ-1129 shows Ki values of 159 and 24 nM for 5-HT1A receptor and D2 receptor. PZ-1129 can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 13.7 nM). PZ-1129 can be used for the research of emotional disorders, such as depression and bipolar disorder.

Pyridine-3-sulfonyl chloride belongs to the substituted sulfonyl chloride class. Due to its high proton affinity, it can be used as a derivatizing agent.

PXS 64, a mannose-6-phosphate (M6P) analogue. a lipophilic prodrug of PXS 25. PXS 64 is an effective anti-fibrotic agent by inhibiting the activation of latent TGF-β1. PXS64, inhibits fibrosis via TGF-β1 pathway in human lung fibroblasts. PXS 64 reduces TGFβ-mediated collagen IV, fibronectin, MCP-1, and phospho-smad2 expression in kidney cells. PXS 64 reduces collagen deposition in dermal scar fibroblasts. PXS 64 can be used for the research of chronic kidney disease, idiopathic pulmonary fibrosis, scarring.

PXS 25 is a cation-independent mannose 6-phosphate receptor (CI-M6PR) inhibitor that inhibits CI-M6PR-mediated activation of latent TGF-β1. PXS 25 inhibits conversion of high glucose-induced latent TGF-β1 to active TGF-β1 in proximal tubule cells under normoxic conditions. PXS 25 suppresses high glucose-induced fibronectin, collagen IV production, and phosphorylated Smad 2 in proximal tubule cells under normoxic conditions. PXS 25 has antifibrotic properties in skin fibroblasts. PXS 25 can be used for the research of diabetic nephropathy.

PU-11 is a Hsp90α/Hsp90β inhibitor with IC50 values of 18.6 μM and 89.8 μM and Kd values of 2 and 4.2 μM. PU-11 binds to the ATP-binding pocket of Hsp90α and Hsp90β and displays selective binding preference for Hsp90α over Hsp90β, mediated by the nonconserved Hsp90α Ser52 residue. PU-11 can be used for the research of neurodegenerative disorders.

PTPN2-IN-3 (example 52) is a PTPN2 inhibitor that can be used in tumor research.

PTPN2-IN-2 is a potent and orally active PTPN2 inhibitor (IC50 = 7.05 nM) that enhances the IFN-γ signaling pathway. PTPN2-IN-2 inhibits PTP1B with an IC50 of 9.88 nM. PTPN2-IN-2 inhibits tumor growth, promotes the activation and infiltration of tumor immune cells in a B16-OVA mouse model. PTPN2-IN-2 can be used for the research of melanoma.

p-Toluenesulfonamide-15N is the 15N-labeled p-Toluenesulfonamide. p-Toluenesulfonamide is an intermediate and plasticizer. p-Toluenesulfonamide is also the main degradation product of the disinfectant Chloramine-T in water. p-Toluenesulfonamide facilitates the localization of fluorescent probes to the endoplasmic reticulum.

PTH1R agonist 4 (Example 63) is a parathyroid hormone 1 receptor (PTH1R) agonist with a pEC50 value greater than 7. PTH1R agonist 4 can be used for the study of bone diseases, such as osteoporosis.

PTH1R agonist 1 (Example 2) is a parathyroid hormone 1 receptor (PTH1R) agonist. PTH1R agonist 1 can be used for research of hypoparathyroidism and osteoporosis.

PTERi is a selective inhibitor of PTER with selectivity towards HDACs. PTERi increases the level of N-acetyltaurine in both lean and obese mice, and reduces food intake in obese mice. PTERi can be used in the research of obesity.

PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC50 of 3 nM. PRT-060318 dihydrochloride suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 dihydrochloride prevents Heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research.

ProX1-(SS)-DOTAGA_R (Compound 25a) is the unbound radionuclide portion of the radiopharmaceutical and can be used for targeted delivery to diseases characterized by ACP3 expression.

Proteasome-IN-1 (Compound 130) is a proteasome inhibitor. Proteasome-IN-1 exhibits antiparasitic activity against P. faciparum 3D7.

PROTAC TG2 Degrader-3 is a TG2 PROTAC degrader. PROTAC TG2 Degrader-3 inhibits the adhesion and migration of ovarian cancer cells. PROTAC TG2 Degrader-3 can be used for the research of ovarian cancer. (Pink: Transglutaminase ligand ; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker ).

PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma. (Pink: TEAD1 ligand ; Blue: Cereblon ligand ; Black: linker ).

PROTAC STAT6 degrader-4 (Compound 3u247) is a STAT6 PROTAC degrader with a DC50 of 0.04 nM. PROTAC STAT6 degrader-4 promotes the ubiquitination and degradation of STAT6, and is applicable to the research of immune diseases.

PROTAC STAT6 degrader-2 is a highly efficient PROTAC degrader targeting STAT6. PROTAC STAT6 degrader-2 has a DC50 value of 1-10 nM for STAT6 in human PBMC cells and a DC50 value of less than 100 nM for STAT6 in HEK293-HIBiT-STAT6 cells. PROTAC STAT6 degrader-2 can be used for STAT6-mediated diseases.

PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers. (Pink: Epigenetic Reader Domain Target protein ligand; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker).

PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research. (Pink: COX and NF-κB ligand ; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker ).

PROTAC SARS-CoV-2 Mpro degrader-8 is an antiviral PROTAC degrader targeting the SARS-CoV-2 main protease (Mpro), with weak direct binding affinity to Mpro (Kd=80.5 μM). PROTAC SARS-CoV-2 Mpro degrader-8 exhibits broad-spectrum antiviral activity against SARS-CoV-2 and the human endemic coronavirus HCoV-OC43. It can be used for research on coronavirus infections. (Pink: SARS-CoV Target protein ligand; Blue: VHL ligand ; Black: ).