Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes.

Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation. Eptifibatide prevents binding of the adhesion proteins fibrinogen and von Willebrand factor to GPIIb/IIIa on the surface of activated platelets to prevent aggregation and thrombus formation. It inhibits ADP-induced citrated blood aggregation (IC50 = 0.11-0.22 μg/ml) in vitro and in vivo (IC50 = 52 μg/ml in porcine plasma). Formulations containing eptifibatide have been used to reduce risk of thrombolysis in myocardial infarction in patients undergoing percutaneous coronary intervention.

An immunoactive peptide that has been shown to inhibit cell proliferation and induce apoptosis in human leukemia, non-small cell lung cancer, melanoma, and other human cancers.

Atosiban (RW22164; RWJ22164) is indeed a nonapeptide and a competitive antagonist of the vasopressin and oxytocin receptors. It is structurally similar to oxytocin but lacks the amino group at the N-terminus, making it a desamino-oxytocin analogue. Atosiban is primarily used as a tocolytic agent, which means it helps to inhibit premature labor by blocking the action of oxytocin on the uterus. This makes it particularly valuable in the management of spontaneous preterm labor, as it can help delay delivery, providing critical time for administering corticosteroids to enhance fetal lung maturity or for transferring the mother to a facility with appropriate neonatal care.

CMP05-7 (Endosomolytic compound CMP05-7) is a novel endosomolytic small-molecule compound that exhibits higher transfection efficiency/ability to induce endosomal escape of oligonucleotides (ONs) than current compounds such as chloroquine.

XST-20 is a small molecule that selectively targets the DNA-binding domain (DBD) of FOXM1, atranscription factor involved in cell cycle progression, proliferation, and cancer development. Witha surface plasmon resonance (SPR)-derived binding affinity (Kd) of 20 uM, XST-20 effectivelysuppresses FOXM1's transcriptional activities, making it a promising candidate for targetingFOXM1-driven cancers, such as ovarian cancer.

JNJ525 is a small molecule inhibitor that targets tumor necrosis factor alpha (TNFα), a cytokine involved in inflammation and immune regulation. TNFα exerts its biological effects by binding to its receptors, TNFR1 (TNF receptor 1) and TNFR2 (TNF receptor 2). JNJ525 works by preventing the formation of TNFα complexes with these receptors, thereby inhibiting TNFα-mediated signaling pathways.

PRLX 93936 is a structural analogue of erastin with potential antineoplastic activity. Erastin analogue PRLX 93936 appears to inhibit mitochondrial outer membrane protein VDACs (voltage-dependent anion channels) 2 and 3, resulting in an oxidative, non-apoptotic cell death. Erastin analogue PRLX 93936 exhibits greater lethality in cell lines harboring mutations in the GTPase protein oncogenes HRAS and KRAS or the serine-threonine protein kinase oncogene BRAF than in non-tumorigenic cell lines. VDACs 2 and 3 are up-regulated in a wide variety of tumor cell lines.

OAT-177 is a potent, selective, orally active acidic mammalian chitinase (AMCase) inhibitor with IC50 of 14 and 19 nM against human and mouse AMCas, respectively, >150-fold selectivity over mCHIT1.

Laduviglusib (CHIR-99021) trihydrochloride is a well-characterized small molecule inhibitor that specifically targets glycogen synthase kinase-3 alpha and beta (GSK-3α/β). It exhibits potent inhibitory activity with IC50 values of 10 nM for GSK-3α and 6.7 nM for GSK-3β. Importantly, it demonstrates high selectivity, being over 500-fold more selective for GSK-3 compared to other kinases such as CDC2 and ERK2, as well as a broad range of other protein kinases.

H-Ile-Pro-Pro-OH, a milk-derived peptide, inhibits angiotensin-converting enzyme (ACE) with an IC50 of 5 μM. Antihypertensive tripeptides.

EP055 (EP-055) is a small molecule that targets EPPIN on the surface of sperm and inhibits motility (IC50=199.5 uM, CASA assay using human sperm), binds to the C-terminal domain of EPPIN.

MTX-3937 is a small-molecule inhibitor targeting Siglec-9 (Sialic acid-binding immunoglobulin-type lectin-9), a member of the Siglec family of immunomodulatory receptors. Siglec-9 is primarily expressed on immune cells, such as myeloid cells and natural killer (NK) cells, and plays a role in regulating immune responses by transmitting inhibitory signals through its intracellular immunoreceptor tyrosine-based inhibitory motifs (ITIMs).

BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells.

PF-07104091 hydrate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E1-amplified cancers.

PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC.

NCA029 is a potent and selective homo sapiens caseinolytic protease P (HsClpP) activator with an EC50 of 0.15 μM. NCA029 acts on HsClpP to activate an ATF3-dependent integrative stress response, leading to colon cancer cell death.

TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. TIM-098a has no inhibitory activity against CaMKK isoforms. TIM-098a inhibits AAK1-regulated endocytosis by suppressing AAK1 kinase activity.

Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research.

MCTR3 is a potent cytokine of pro-resolving mediating maresin conjugates in tissue regeneration (MCTR), which reduces the inflammatory response and promotes the tissue regeneration. MCTR3 exhibits potency in ameliorating LPS-induced acute lung injury and arthritis.

LW-216 is a TrxR1 inhibitor that induces Apoptosis. LW-216 has anti-tumor activity.

CGP36216 hydrochloride is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders.

ODN 1668 sodium, a class B CpG ODN (oligodeoxynucleotide), is a TLR-9 agonist. ODN 1668 sodium is an immunostimulatory sequence and can be used as vaccine adjuvant. Sequence: 5'-tccatgacgttcctgatgct-3’.

Cosdosiran is a chemically modified siRNA designed to temporarily inhibit expression of the caspase 2 protein and can be used for the study of nonarteritic anterior ischemic optic neuropathy and other optic neuropathies such as glaucoma that result in the death of retinal ganglion cells.

ODN 2088 sodium is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 sodium shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.

Polyinosinic acid sodium is the sodium form of Polyinosinic acid. Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) ligand. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation.

SPC5001 sodium is a locked nucleic acid (LNA)-modifed antisense oligonucleotide (ASO) complementary to human PCSK9 (proprotein convertase subtilisin/kexin type 9) mRNA. SPC5001 sodium can be used for the research of hypercholesterolemia. SPC5001 sequence: 5′-TGmCTACAAAACmCmCA-3′.

ARC19499 sodium is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 sodium blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 sodium corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.

Remlarsen (MRG-201), a miR-29b mimic, acts a miR-29b agonist. Remlarsen sodium has the potential for preventiong formation of a fibrotic scar or cutaneous fibrosis.

Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model.