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.

RIPK1-IN-34 is a selective, brain-penetrant RIPK1 inhibitor (IC50 = 126.70 nM) with almost no inhibitory effect on RIPK3 (IC50 ＞ 10, 000 nM). RIPK1-IN-34 offers substantial neuroprotection by inhibiting the phosphorylation of RIPK1, RIPK3, and mixed lineage kinase domain-like pseudokinase (MLKL) within the necroptosis pathway. RIPK1-IN-34 shows the neuroprotective effect in a rat middle cerebral artery occlusion (MCAO) model. RIPK1-IN-34 can be used for the study of anti-acute ischemic stroke (AIS).

Rimegepant (BMS-927711) hemisulfate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor. Rimegepant hemisulfate can be used for migraine research.

RIG 200 is an S-nitrosothiol nitric oxide (NO) donor. RIG 200 releases NO through decomposition, activating guanylate cyclase (sGCM) in vascular smooth muscle cells, increasing cGMP levels, and leading to vasodilation. RIG 200 significantly inhibits Collagen-induced platelet aggregation in platelet-rich plasma (PRP). RIG 200 may be used in research on antithrombus.

Rhodexin A is a cardenolide. Rhodexin A can be isolated from the extract of Rhodea japonica. Rhodexin A induces Apoptosis. Rhodexin A exerts a digitalis-like action in the cat heart. Rhodexin A has anticancer activity against leukemia.

RhlR agonist-1 is a N-acylated L-homoserine lactone and is a selective quorum sensing receptor RhlR agonist. RhlR agonist-1 can be used for the research of bacterial infections.

RH01504 is a HIF2α inhibitor with a Kd value of 5.42 nM against human HIF2α. RH01504 inhibits the growth of renal cancer cells. RH01504 can be used in research related to renal cell carcinoma.

RGA-C11 is a detergent.

RG3039 hydrochloride is an orally active, blood-brain barrier-permeable DcpS inhibitor with an IC50 of 4.2 nM against hDcpS. RG3039 hydrochloride inhibits the decapping activity of DcpS and maintains DcpS in a catalytically inactive conformation in the central nervous system and other tissues. RG3039 hydrochloride extends survival and improves function in spinal muscular atrophy mice. RG3039 hydrochloride is applicable to research related to spinal muscular atrophy.

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).

Rezatapopt analog-1 (PC14586 analog-1) (1919) is a Rezatapopt analog. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure.

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.

Rev1-CT/RIR PPI-IN-1 (Compound 1) is a thiophene-based compound. Rev1-CT/RIR PPI-IN-1 can specifically disrupt the protein-protein interaction between Rev1-CT and RIR, with an IC50 value of 2.5 µM. Rev1-CT/RIR PPI-IN-1 can enhance chemosensitivity and reduce the mutation rate in Cisplatin-sensitive HT-1080 cells. Rev1-CT/RIR PPI-IN-1 can be used for tumor research.

Retro-1 is a toxin inhibitor. Retro-1 blocks the retrograde transport of STxB to the trans-Golgi network/Golgi. Retro-1 inhibits the cytotoxic effects of Ricin, bacterial toxins Stx1 and Stx2. Retro-1 can also substantially enhance the effectiveness of antisense and splice switching oligonucleotides.

RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC50s: 1.4 nM, 1.9 nM, 3.8 nM for RETWT, RETV804L, RETV804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC50s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers.

Renin-IN-4 is a Renin inhibitor. Renin-IN-4 can be used for the research of cardiovascular disease.

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.

rel-ML123 is a negative control probe of ML123 (trans-Racemate).

rel-Latanoprost acid is a relative configuration of Latanoprost acid. Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.

rel-CTR/AMYR agonist-1 (Example 169) is an agonist of amylin and/or calcitonin receptor.

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.

RB-105 is an inhibitor of angiotensin-converting enzyme (ACE) (Ki = 4.2 nM) and neutral endopeptidase (NEP) (Ki = 1.7 nM). RB-105 after inhibiting ACE reduces the production of Ang II and increase the level of bradykinin. RB-105 after inhibiting NEP increases the level of natriuretic peptide and further increases the level of bradykinin, thereby generating a powerful synergistic effect. RB-105 has significant antihypertensive and natriuretic effects in both spontaneously hypertensive rats and normal blood pressure rats. RB-105 can be used for research on hypertension.

Rapamycin-butyl ester (Sirolimus-butyl ester) (Compound 9) is a derivative of Rapamycin. Rapamycin-butyl ester exhibits antiproliferative effects against liver cancer cells and renal cancer cells. Rapamycin-butyl ester can be used in research related to liver cancer and renal cancer.

RANKL-IN-2 is an orally active RANKL inhibitor with Kd values of 3.21 μM and 4.625 μM in the SPR and MST assays, respectively. RANKL-IN-2 binds to RANKL to interfere with RANKL-RANK interaction. RANKL-IN-2 suppresses osteoclastogenesis by inhibiting ROS, MAPK and NF-κB pathways. RANKL-IN-2 inhibits osteoclastogenesis via inhibition of RANKL-induced osteoclast formation, bone resorption, and osteoclast-specific gene and protein expressions in vitro.RANKL-IN-2 prevents bone loss in ovariectomized osteoporosis mice.RANKL-IN-2 can be used for the research of osteoporosis.