RO-4597014 is a glucokinase inhibitor. RO-4597014 can be used in the study of diabetes.

Ro 23-7553 is a mitochondrial inhibitor. Ro 23-7553 promotes chondrocyte differentiation at physiological concentrations, while supraphysiological concentrations inhibit both proliferation and differentiation. Ro 23-7553 can be used for the study of cancer.

RIPK1-IN-38 is an orally active RIPK1 inhibitor with an IC50 value of 27 nM. RIPK1-IN-38 can inhibit the phosphorylation of RIPK1 and its downstream signaling molecules RIPK3 and MLKL. RIPK1-IN-38 exhibits anti-necroptotic activity. RIPK1-IN-38 has excellent anti-inflammatory efficacy in both the SIRS model and GVHD model. RIPK1-IN-38 can be used for the research of inflammatory and immune-related diseases.

RIPK1-IN-36 (Example 4.1) is a RIPK1 inhibitor with an EC50 of <25 nM. RIPK1-IN-36 can be used for the study of RIPK1-related diseases.

RGA-C11 is a detergent.

Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib hydrochloride exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib hydrochloride has excellent central nervous system (CNS) penetration and has antitumor activity, such as non-small cell lung cancer (NSCLC).

Rev1-CT/RIR PPI-IN-2 (compound 10) is a Rev1-CT/RIR protein-protein interaction inhibitor.Rev1-CT/RIR PPI-IN-2 enhances cisplatin-mediated cell killing.

Renin IN-2 (compound 27) is a human renin inhibitor with an IC50 of 0.059 μM. Renin IN-2 exhibits oral efficacy. Renin IN-2 can be used in the research of hypertension.

RdRP-IN-10 is a SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor with an IC50 value of 5.78 μM. RdRP-IN-10 forms covalent binds with SARS-CoV-2 nsp8 Cys114, disrupts nsp8-nsp12 stabilizing interactions. RdRP-IN-10 inhibits SARS-CoV-2 RdRp-mediated RNA polymerization without interfering with RNA-RdRp complex binding. RdRP-IN-10 exerts antiviral effects in cellular models. RdRP-IN-10 can be used for the research of SARS-CoV-2 infection.

RBP4-IN-3 (Compound 38) is a retinol-binding protein 4 (RBP4) inhibitor. RBP4-IN-3 can be used in studies related to cardiovascular diseases and obesity.

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.

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

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.

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.

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.

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 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 mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin (mHTT) PROTAC degrader. PROTAC mHTT Degrader-1 specifically recognizes pathogenic mHTT aggregates and recruits Cereblon (CRBN), thereby inducing ubiquitination and proteasomal degradation of mHTT. PROTAC mHTT Degrader-1 alleviates mHTT-induced cytotoxicity and neuroinflammation. In the R6/2 Huntington's disease mouse model, PROTAC mHTT Degrader-1 reduces cerebral protein aggregation levels and improves body weight, motor coordination and survival rate of animals. PROTAC mHTT Degrader-1 can be used for research on PROTAC therapies for Huntington's disease and other neurodegenerative diseases. (Pink: Huntingtin ligand ; Blue: Cereblon ligand ; Black: linker ).

PROTAC LRRK2 Degrader-1 (compound 18) is a leucine-rich repeat kinase 2 (LRRK2) PROTAC degrader with an IC50 value less than 10 nM. PROTAC LRRK2 Degrader-1 can be used in the research of Parkinson's disease.

PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII. (Pink: CA Ⅱ ligand ; Blue: Cereblon ligand ; Black: linker).

PROTAC GPX4 degrader-5 (compound N15) is an efficient and highly selective PROTAC GPX4 degrader (DC50 = 28 nM). PROTAC GPX4 degrader-5 can induce ferroptosis and has low toxicity to normal cells. PROTAC GPX4 degrader-5 can significantly increase ROS. PROTAC GPX4 degrader-5 exerts anti proliferative effects on various tumor cells. PROTAC GPX4 degrader-5 is commonly used in cancer research. (Pink: GPX4 ligand ; Blue: Others ligand ; Black: linker ).

PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer. (Pink: EZH2 ligand ; Blue: VHL ligand ; Black: linker).

PROTAC EZH2 Degrader-42 (compound 57) is an EZH2-targeting PROTAC degrader and antiproliferative agent. PROTAC EZH2 Degrader-42 induces cIAP-mediated ubiquitination and subsequent proteasomal degradation of EZH2. PROTAC EZH2 Degrader-42 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Aminopeptidase ligand ; Black: linker).

PROTAC EZH2 Degrader-41 is an EZH2-targeting PROTAC and cIAP E3 ubiquitin ligase recruiter. PROTAC EZH2 Degrader-41 induces EZH2 degradation via ubiquitination and proteasomal breakdown. PROTAC EZH2 Degrader-41 exerts antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: cIAP ligand ; Black: ).

PROTAC EZH2 Degrader-31(compound 69) is a PROTAC protein degrader targeting EZH2, with antiproliferative IC50 values of 3.63 μM in lSU-DHL-6 cells and 8.74 μM in HBL-1 cells. PROTAC EZH2 Degrader-31 can be used for the research of lymphoma. (Pink: EZH2 ligand ; Blue: MDM2 ligand ; Black: linker).

PROTAC EZH2 Degrader-17 (compound 52) is a PROTAC protein degrader targeting EZH2 with an antiproliferative IC50 of 18.32 μM in lymphoma cells. PROTAC EZH2 Degrader-17 exhibits antiproliferative activity against lymphoma cells. PROTAC EZH2 Degrader-17 can be used for the research of lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).