Saframycin S is an antibiotic with a racemomycin group that exhibits inhibitory activity against Ehrlich ascites tumors. The LD50 of Saframycin S in ddY mice is 3.2 mg/kg (i.p.).

S3226 is an inhibitor for Na+/H+ exchange subtype 3 (NHE3) with an IC50 of 0.2 µmol/L in rat NHE3 transfected fibroblasts. S3226 exhibits protective activity in rat ischemia-induced acute renal failure models.

S118 is an orally active sphingosine-1-phosphate receptor 2 (S1P2 receptor) inhibitor. S118 prevents the binding of the S1P2 receptor to dapper1 (Dpr1), reduces the accumulation of β-catenin and blocks the nuclear translocation of the S1P2 receptor, thereby inhibiting inflammation, fibrosis, and epithelial-mesenchymal transition (EMT) and exerting anti-idiopathic pulmonary fibrosis (IPF) activity. S118 is promising for research of idiopathic pulmonary fibrosis.

RuDiOBn scanvages DPPH and ABTS free radicals (13.2% and 5.9% clearance at 100 μg/mL), exhibits low antioxidant activity. RuDiOBn inhibits the collagen glycation, reduces the formation of advanced glycation end products (AGEs) with an IC50 of 2.45 μg/mL. RuDiOBn enhances the proliferation and migration of fibroblasts, stimulates the synthesis of collagen, promoting the skin repair and regeneration. RuDiOBn also inhibits collagenase.

RU26988 is a highly specific glucocorticoid receptor agonist with a very low affinity for salocorticoid receptors.

RU 26752 is a steroid hormone receptor antagonist. RU 26752 can prevent hypertension caused by aldosterone with antitumor activity. HYS-072 induces apoptosis and autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway and suppresses tumor growth in vivo in xenograft models by modulating autophagy-related pathways. HYS-072 can be used in the research of triple-negative breast cancer.

RS-57067 is a COX-2 inhibitor with a Ki of 16.9 μM. RS-57067 reduces the production of prostaglandins (such as PGE2) by inhibiting COX-2, thereby alleviating the inflammatory response. RS-57067 can be used in the research of inflammatory and immune diseases.

ROS inducer 9 (compound 4e) is an antibacterial agent with a MIC value of 0.25 μg/mL against E. coli. ROS inducer 9 kills bacteria by inhibiting GSH activity and increasing ROS levels. ROS inducer 9 shows low toxicity to erythrocytes and RAW 264.7 cells.

Rofleponide 21-palmitate is a synthetic glucocorticoid.

Rocavorexant is the antagonist for orexin-1 receptor with pIC50 of 9.1 for human OX1 (while pIC50 for human OX2 is 6.0).

Ro26-4550 TFA is a low micromolar antagonist of IL-2/IL-2Rα binding with an IC50 value of 3 μM.

RNA recruiter-linker 1 is the RNA ligand-linker part of RNAse L RIBOTAC. H117 has competitive binding and inhibition ability on SARS-CoV-2 main protease (Mpro) with an IC50 of 151.3 nM.

RNA recruiter 1 is the RNA ligand of RNAse L RIBOTAC.

RK-0080552 (RK-552) is a NSD2 histone methyltransferase inhibitor. RK-0080552 demonstrates significant cytotoxicity against multiple myeloma (MM) cells carrying t(4;14). RK-0080552 suppresses the IRF4 gene, reducing the level of histone H3 lysine 36 dimethylation. RK-0080552 is promising for research of hematological malignancies.

Rezuforimod is the agonist for N-formyl peptide receptor like-1 receptor (FPRL-1) with an EC50 of 0.88 nM in CHO-Ga16 cell. Rezuforimod exhibits anti-inflammatory activity.

rel-Hydroxy Itraconazole (rel-R-63373) is a relative stereoisomer of Hydroxy Itraconazole. Hydroxy Itraconazole is the major active metabolite of the antifungal compound Itraconazole. Enterobactin is a bacterial siderophore that promotes iron absorption.

RBx-0597 is a potent and selective DPP-IV inhibitor, demonstrating IC50 values of 32, 31, and 39 nM against human, mouse, and rat plasma DPP-IV, respectively. RBx-0597 shows potential for type 2 diabetes research.

RA-PR058 is an orally active Ramalin derivative with blood-brain barrier permeability, exhibiting multi-target regulatory effects and favorable pharmacokinetic properties. RA-PR058 demonstrates potential as a multi-target modulator for Alzheimer's disease by reducing the expression of BACE1, tau protein hyperphosphorylation, and anxiety-like behaviors.

Rapaglutin E (RgE) is a glucose transporter (GLUT) inhibitor. Rapaglutin E exhibits dose-dependent inhibition of [3H]-2DG uptake in A549, Jurkat T, PANC10.05, and RBC, with IC50 values 8.9 nM, 3.1 nM, 35.5 nM, 74.2 nM. Rapaglutin E inhibits cell proliferation in A549, PANC10.05, HeLa, Jurkat T, and HEK293T cells.

Rapaglutin A is a glucose transporter (GLUT) inhibitor. Rapaglutin A is a pan-GLUT inhibitor of Class I isoforms GLUT1, GLUT3, and GLUT4 with an IC50 of 12 nM. Rapaglutin A has an inhibitory effect on A549 proliferation.

QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively.

QKY-613 is a prodrug that enhances immune surveillance by targeting nucleic acid modification pathways. QKY-613 promotes the selective incorporation of 6mdA (N6-methyldeoxyadenosine) into viral DNA, enhancing the phase separation potential of DNA, thereby increasing the activation of cGAS and strengthening host immune surveillance. In virus-infected mouse models, QKY-613 significantly reduced mortality in aged mice. QKY-613 holds promise for research on nucleic acid modification-based immune surveillance mechanisms.

QI-18 is a fibroblast activation protein (FAP) inhibitor with the IC50 of 0.50 nM, which is a 6.5-fold increase in potency over that of UAMC-1110 (IC50 of 3.25 nM). QI-18 can be used to synthesize high tumor selectivity and high dose radiotracers for the diagnosis and treatment of tumors.

Pyrithyldione is a sedative-hypnotic agent that induces agranulocytosis.

Pyridyl disulfide-Dexamethasone is a Dexamethasone in rats. p-MPPF can be used for neurological disease research.

PTX80 is an antagonist of p62 with an IC50 value of 31.18 nM. PTX80 reduces tumor volume in an HCT116 colorectal cancer mouse xenograft model.

PTP1B/TC-PTP IN-1 is a PTP1B and TC-PTP dual inhibitor. PTP1B/TC-PTP IN-1 can be used as a target protein ligand for the synthesis of DU-14 (PTP1B/TC-PTP PROTAC).

PTC-700 is a potent microtubule-associated protein tau (MAPT) splicing modulator. PTC-700 reduces 4R MAPT in both P301L and S305N neurons with EC50s of 1.3-1.8 nM, and 0.5-2.6 nM, respectively.

PST3.1a is a N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with the IC50 of 2 μM. PST3.1a inhibits glioblastoma-initiating cell invasiveness and proliferation.

PSMA precursor-1 is a precursor in the synthesis of prostate-specific membrane antigen (PSMA) ligands and fluorescent probes that have been used in the detection of PSMA in LNCaP and PC3 cells.