SARM1-IN-9 (Compound MY-13B) is a stereoselective SARM1 inhibitor. SARM1-IN-9 is applicable to research related to axon degeneration-dependent neurological diseases.

SAR113945 (compound 1) is a highly potent IKK-β inhibitor with an IC50 of 0.4 nM. SAR113945 is used for research on inflammatory and cancerous diseases.

Sapunifiram is a cognitive enhancer. Sapunifiram can be used in studies related to amnesia.

Sameridine (NIH-10908 free base) is a weak partial agonist of the μ-opioid receptor. Sameridine shows local anesthetic and analgesic properties. Sameridine has minimal respiratory depression at low doses, but can suppress ventilatory response at high doses. Sameridine can be used for the study of analgesic effect.

Salanersen is an antisense oligonucleotide targeted to survival motor neuron 2 (SMN2). It is used for the study of spinal muscular atrophy (SMA).

S-Adenosyl-L-ethionine is S-Adenosyl-L-methione analog. S-Adenosyl-L-ethionine is able to replace S-Adenosyl-L-methione during HydG catalysis. HydG can utilize S-Adenosyl-L-ethionine as an effective alternative cosubstrate to S-Adenosyl-L-methione under normal enzymatic turnover conditions, producing the Ω intermediate and allowing efficient catalytic turnover of substrate L-tyrosine.

Saccharolactone is a potent orally active β-glucuronidase inhibitor. Saccharolactone markedly lowers biliary endogenous β-glucuronidase activity in the rat bile. Saccharolactone can stabilize glucuronide metabolites in vitro. Saccharolactone is also a strong inhibitor of CYP1A2, 2D6, 3A4 and 2C8 isoforms (IC50 < 4 mM).

S-8666 is an orally active uricosuric antihypertensive diuretic. The S-8666 has both S-(-)- and R-(+)-isomers. The diuretic and sodium-excretion activities of it are entirely dominated by the S-(-)-isomer, while the R-(+)-isomer shows no significant activity. S-8666 relies on the organic acid transport system to be secreted through the proximal tubule. S-8666 exhibits a clear uric acid excretion-promoting activity and diuretic effect in various species (such as rats and chimpanzees).

S1R agonist 3 is a potent and selective sigma-1 receptor (S1R) agonist with a Ki of 1.5 nM. S1R agonist 3 reduces hyperlocomotion in wfs1abKO zebrafish larvae without affecting locomotion in wildtype wfs1abWT zebrafish larvae. S1R agonist 3 reverses Aβ25-35-induced learning and memory impairments. S1R ligand 1 can be used for the research of Alzheimer’s disease.

S1PR1/S1PR5 agonist-1 (Compound 19) is an orally active S1PR1 and S1PR5 agonist with EC50 values of 40.0 and 22.9 nM, respectively. S1PR1/S1PR5 agonist-1 binds to key residues of S1PR1 to mediate agonistic activity. S1PR1/S1PR5 agonist-1 alleviates colitis pathological changes in DSS-induced mouse models and exerts minimal effects on mouse heart rate. S1PR1/S1PR5 agonist-1 can be used for the research of inflammatory bowel disease.

S1PR1 agonist 3 (Compound Y18) is a highly selective S1PR1 receptor agonist (EC50=0.98 nM). S1PR1 agonist 3 is promising for research of autoimmune diseases such as multiple sclerosis and ulcerative colitis.

RX-RA-69 is an orally active platelet phosphodiesterase (PDE) inhibitor with a IC50 of 1 nM. RX-RA-69 elevates cAMP levels in platelets, exerts anti-aggregatory effects, and inhibits the formation of coronary platelet thrombi. RX-RA-69 exhibits anti-metastatic activity in a mouse Lewis lung cancer model. RX-RA-69 can be used in research related to coronary platelet thrombi and Lewis lung cancer.

RU 56279 is an androgen receptor (AR) antagonist with strong and systemic anti-androgenic activity. RU 56279 is also a common, potent and long-lasting anti-androgen metabolite of RU 56187 and RU 58841 in vivo. RU 56279 can be used as an AR ligand to construct an AR-targeted prodrug system for the study of AR-positive tumor cells.

RSK4-IN-2 (compound 16o) is a potent, orally active RSK4 inhibitor with an IC50 of 17 nM. RSK4-IN-2 suppresses esophageal squamous cell carcinoma (ESCC) cell growth and invasion, by inhibiting phosphorylation of RSK4 downstream targets. RSK4-IN-2 inhibits tumor growth and metastasis in ESCC mouse models. RSK4-IN-2 can be used for ESCC research.

RPR-200765A methanesulfonate is an orally active p38 MAPK inhibitor with an IC50 of 0.050 μM. RPR-200765A methanesulfonate shows weak activity against Lck, and exhibits no significant activity against ERK, ZAP70 or SYK. It inhibits the production of TNFα and can be used in the research of inflammatory diseases.

Rosuvastatin TMBA (ZD 4522 TMBA) is a drug impurity.

Rosellichalasin is an antibacterial agent isolated from the endophytic fungus Aspergillus flavipes Y-62. Rosellichalasin exhibits antibacterial activity.

RORγt inverse agonist 36 (S configuration of Compound 16) is a RORγt inverse agonist. RORγt inverse agonist 36 can be used for the research of inflammation and immunology.

Ronomilast (Elbimilast; ELB353) is an orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 3 nM. Revamilast can be used for research to inflammation related diseases.

ROCK2-IN-14 is an orally active, selective ROCK2 inhibitor (IC50=4.8 nM) with 212-fold selectivity over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 downregulates S100A9 expression, inhibits NM2 phosphorylation and restores cytoskeletal abnormalities. Furthermore, ROCK2-IN-14 reduces inflammatory cytokine levels, alleviates skin inflammation and exerts anti-inflammatory activity. ROCK2-IN-14 also significantly inhibits ear thickening in a mouse model of atopic dermatitis (AD), and decreases the levels of IgE, TNF-α, IL-6 and TSLP. ROCK2-IN-14 has a good safety profile, with a maximum tolerated oral dose exceeding 500 mg/kg. ROCK2-IN-14 can be used for research on atopic dermatitis.

Ro-65-3479 is a selective metabotropic glutamate receptor (mGlu2/3) antagonist. Ro-65-3479 blocks glutamate-induced signaling and modulates calcium channel activity. Ro-65-3479 is promising for research of disorders involving glutamatergic dysregulation, such as anxiety, schizophrenia, and neurodegenerative diseases.

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.

RNA polymerase-IN-4 is a RNA polymerase inhibitor with an EC50 of 22.81 nM. RNA polymerase-IN-4 exhibits potent anti-influenza virus activity (EC50 = 3.76 nM), relatively low cytotoxicity (CC50 = 29.91 μM). RNA polymerase-IN-4 can be used for the research of infection, such as influenza virus infection.

RM-046 is an orally active, selective ternary complex inhibitor of KRASQ61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRASQ61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRASQ61H mutant cancers.

RM-041 is a selective, orally active KRASG13C (ON) inhibitor that forms a covalent complex with KRASG13C (ON) and Cyclophilin A. RM-041 blocks the binding of RAS effector proteins via steric hindrance, and then covalently binds to Cys-13 to form an irreversible inhibitory complex, thereby inhibiting the proliferation of KRASG13C mutant cancer cells. RM-041 induces regression of KRASG13C tumors in cellular and xenograft tumor models. RM-041 exerts a synergistic effect when combined with upstream node inhibitors (such as SHP2 inhibitors). RM-041 can be used for the research of non-small cell lung cancer.

RIPK1-IN-39 (compound 2) is a potent and selective RIPK1 inhibitor (IC50 = 69.40 nM) exhibiting >100-fold selectivity over RIPK3 (IC50 = 6946 nM). RIPK1-IN-39 protects HT-22 and HT-29 cells from necroptosis by inhibiting the phosphorylation and activation of the RIPK1-RIPK3-MLKL pathway. RIPK1-IN-39 demonstrates neuroprotective effects in a rat model of middle cerebral artery occlusion (MCAO). RIPK1-IN-39 can be used for acute ischemic stroke (AIS) research.

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-37 is an RIPK1 inhibitor and a ligand for the target protein for PROTAC LD5097. RIPK1-IN-37 can be used to synthesize PROTAC. (Pink: RIPK1 ligand ; Blue: VHL ligand ; Black: linker ).

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.