RG7109 is an inhibitor of HCV NS5B polymerase. RG7109 has EC50 values of 1.1 nM and 1.0 nM for HCV GT-1a H77 and GT-1b Con1, respectively. RG7109 exhibits favorable pharmacokinetic properties and can be used in anti-HCV research.

BMS-210285 is a highly selective agonist for the β3 receptor. BMS-210285 can be studied for obesity and type 2 diabetes research.

Apicidin C (Compound 5a) is a cyclic tetrapeptide. Apicidin C has an antiprotozoal and antimalarial activity against Eimeria tenella (IC50: 6 nM) by reversibly inhibiting HDAC acyivity. Apicidin C can be used for malaria infections research.

4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE is a drug-linker conjugate for ADC. 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE contains a linker and bioactive small molecule toxins MMAE. 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE can conjugate with NN2101 (anti c-Kit) for synthesizing NN3201. NN3201 rapidly internalizes and inhibits SCF-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models, such as small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST).

SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer.

CB2R ligand-1 (Compound L14) is a selective Cannabinoid type 2 receptor (CB2R) ligand with a with Ki of 0.16  nM for CB2R over CB1R. CB2R ligand-1 as be used as a tracer for positron emission tomography (PET) imaging of neurodegenerative diseases, inflammation and cancer.

Rodin-B is a selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-B is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.

BMS-577098 is an orally active and ATP-competitive insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 0.016 μM. BMS-577098 shows anti-tumor effect.

UK-315716 is an NMDA receptor antagonist. UK-315716 has a synergistic neuroprotective effect. UK-315716 can be used for research on neurological diseases such as stroke and headache.

FCE-25199 is a novel oral penem antibiotic. FCE-25199 has antibacterial activity against various Gram positive and Gram negative bacteria. FCE-25199 is commonly used in the study of bacterial infections.

SIB 1663 is a conformationally restricted analog of nicotine. SIB-1663 selectively activatedα2β4 and α4β4 human recombinant neuronal nAChRs. SIB 1663 can increase DA and NE release. SIB 1663 can be used for the research of neurological disease.

CP-100356 is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 is also a weak inhibitor of OATP1B1 (IC50 = ∼66 µM). CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM).

UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. UVI3502 blocks Gi/o protein coupling induced by the agonist CP55,940. UVI3502 is promising for research of endocannabinoid system-related diseases in the central nervous system (such as cognitive impairment and neurodegenerative diseases).

G9D-4 (TFA) is a potent PROTAC degrader of G9a, with the DC50 value of 0.1 μM in PANC-1 cells and do not directly perturb GLP protein, with the DC50 of ＞10 μM. G9D-4 (TFA) plays an important role in pancreatic cancer research.

Deoxy-thalidomide-OMe is an E3 ligase ligand. Deoxy-thalidomide-OMe can be used for synthesis of PROTAC LRRK2 Degrader-4.

ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41  nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research.

IP-66 is a potent postsynaptic alpha-receptor antagonist. IP-66 can be used for the research of cardiovascular disease, such as hypertension.

MT-44 is a highly selective and potent mTOR inhibitor with an IC50 of 49.4 nM. MT-44 can inhibit cancer cells proliferation, migration and invasion. MT-44 can induce cells apoptosis and ROS production and cause G2/M phase arrest. MT-44 can activate the cGAS/STING pathway. MT-44 can be used for the research of cancer, such as triple-negative breast cancer.

BJH-86 is a soluble mitochondrial complex 1 inhibitor (oxygen consumption rate inhibition IC50 = 5 μM). BJH-86 exhibits weak inhibitory activity against phosphodiesterase 10A (PDE10A) (IC50 >10 μM). BJH-86 can reduce cellular oxygen consumption and inhibit cancer cell proliferation. BJH-86 can be used for the research of cancer, such as lung cancer.

TPAPyN is a nitroreductase(NTR)-responsive type I photosensitizer. TPAPyN facilitates the imaging of hypoxic cancer cells and image-guided photodynamic therapy (PDT). TPAPyN does not emit fluorescence in the aqueous environment, but restores when NTR cleaves the nitrofuran quencher with aggregation-induced emission. TPAPyN can be used as a fluorescent probe for specific imaging of hypoxic cancer.

CIMBA hydrochloride is a selective G protein-coupled estrogen receptor (GPER) antagonist. CIMBA hydrochloride is used in the research of cholesterol gallstones in women.

SKF-96365 is a blocker of calcium store-operated calcium influx (SOCE) and transient receptor potential channels (TRPC). SKF-96365 reduces the increase in intracellular calcium concentration by blocking TRPC channels and SOCE. SKF-96365 enhances the reverse operation of Na⁺/Ca²⁺ exchanger (NCX) (Ca²⁺ influx) in glioblastoma, leading to intracellular calcium overload and cytotoxicity. SKF-96365 inhibits the CaMKIIγ/AKT pathway and simultaneously induces apoptosis and cell protective autophagy in colorectal cancer cells. SKF-96365 can be used in calcium signaling and cancer research.

UK-78282 is a selective Kv1.3 voltage-gated potassium channel inhibitor with an IC50 of 200 nM. UK-78282 also inhibit Kv1.4 potassium channel. UK-78282 can inhibit human T cell activation.

FHND5071 (1H) is a selective inhibitor targeting the RET (rearrangement during transfection) tyrosine kinase. FHND5071 (1H) is promising for research of RET-driven cancers (such as thyroid cancer, lung cancer, etc.).

DDR1 ligand 1-piperidine is a target protein ligand and linker conjugate, which can be used for the synthesis of PROTAC DDR1 degrader-1.

DDR1 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). DDR1 ligand 1 can be used for the synthesis of PROTAC DDR1 degrader-1.

GRL-07524 (Compound 4e) is a potent inhibitor of HIV-1 protease (Ki = 0.22 nM). GRL-07524 contains oxaspirocyclic carbamates as the P2 ligands. GRL-07524 exhibits good antiviral activity with an EC50 = 210 nM. GRL-07524 binds to the HIV-1 PR active site in one of the four symmetry independent molecules along with key catalytic residues.

CD-10 is an orally active and BBB-penatrable Keap1-Nrf2 protein-protein interaction (PPI) inhibitor. CD-10 binds to Keap1 with a KD value of 193 nM. CD-10 exhibits potent anti-oxidative and anti-inflammatory effects through Keap1-Nrf2 pathway activation, evidenced by reduced levels of MDA, IL-4, IL-10 and increased expression of HO-1. CD-10 effectively alleviated anxiety and depressive behaviors and restored serum neurotransmitter levels by promoting Nrf2 nuclear translocation in the chronic unpredictable mild stress (CUMS) mouse model. CD-10 can be used for the study of depression.

Z55660043 is a Regulator of G protein signaling-14 (RGS14) inhibitor with an IC50 of 2.3  μM. Z55660043 selectively and non-covalently inhibits RGS14 GTPase-accelerating protein (GAP) activity without measurable cytotoxicity. Z55660043 can be used for central nervous system and metabolic disorders research.

KI-DX-014 is a DDX21 inhibitor with an IC50 of 3.31  μM. KI-DX-014 significantly inhibits the DDX21-RNA interaction and modulates ATPase activity and biomolecular condensate formation. KI-DX-014 reduces the DDX21-dependent release of P-TEFb from the 7SK snRNP complex, inhibits P-TEFb-dependent phosphorylation of the RNA polymerase II CTD, and induces developmental defects in zebrafish embryos. KI-DX-014 can be used for cancers and neurodegenerative disorders research.