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.

ZINC13000658 is a METTL inhibitor. ZINC13000658 exhibits significant anti proliferative activity in various cells and can induce G1 phase cell cycle arrest and apoptosis such as HepG2 (IC50 = 5.632 µM) and SNU-449 (IC50 = 6.184 µM) cells. ZINC13000658 may be related to the inhibition of the activity of multiple methyltransferases such as METTL1, 3, 6, 16, 18, etc. ZINC13000658 can be used for research on various types of 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.

VU6080824 (hydrochloride), a derivative of ML-133), is an inward-rectifier potassium channel (Kir2.1) inhibitor with an IC50 of 0.35  μM. VU6080824 (hydrochloride) has superior thallium flux and manual patch clamp (MPC) functional potency.

VU6080824 (Compound 5s), a derivative of ML-133), is an inward-rectifier potassium channel (Kir2.1) inhibitor with an IC50 of 0.35  μM. VU6080824 has superior thallium flux and manual patch clamp (MPC) functional potency.

SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC.

Lin28 degrader MG-Lin3 is a molecular glucose degrading agent that targets the Lin28 protein. Lin28 degrader MG-Lin3 significantly reduces the Renilla luciferase signal at 100 µM. Lin28 degrader MG-Lin3 inhibits the maturation of tumor microRNA let-7. Lin28 degrader MG-Lin3 can be used for cancer research.

5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.

DJ-89 (Compound 77) is a potent soluble epoxide hydrolase (sEH) inhibitor with an IC50 value of 0.51 nM . DJ-89 inhibits sEH from hydrolyzing epoxyeicosatrienoic acids (EETs), reducing the production of pro-inflammatory substances. DJ-89 is promising for research of acute and chronic inflammatory diseases (such as rheumatoid arthritis).