Cleminorexton (Compound 67A) is an agonist of orexin-2 receptor (OX2R). Cleminorexton can be studied in research for narcolepsy and other disorders related to orexin insufficiency and/or excessive sleepness.

17β-HSD5 inhibitor 2 (Compound 30) is an inhibitor for 17β-hydroxysteroid dehydrogenases 5 (17β-HSD 5) with IC50 of 40 nM.

BTX-6654 (formate) is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 (formate) reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations.

TFSeB is an orally active neuroprotective agent. TFSeB can reduce Streptozotocin (STZ)-induced MAO-B and AChE activity. TFSeB exerts neuroprotective effects by increasing the expression of BCL-2, BDNF, NRF2, and decreasing the expression of BAX. TFSeB can reduce lipid peroxidation (TBARS) and reactive oxygen species (ROS) levels. TFSeB can reduce neuroinflammation. TFSeB can be used for research on Alzheimer’s disease.

Gemigliptin (hydrochloride) is the hydrochloride salt of Gemigliptin. Gemigliptin (hydrochloride) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin (hydrochloride) exhibits potent anti-glycation properties. Gemigliptin (hydrochloride) can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

C3TD078 is a WDR5 WIN site inhibitor with a Ki of 0.03  nM. C3TD078 has potent antiproliferative activity and reduces the stem-cell frequency of cancer stem cells (CSCs). C3TD078 can be used for glioblastoma (GBM) research.

Maleimide-Ph(3,5-F)-PEG4-Val-Ala is a cleavable PEG-based ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs).

K2V-9 is an AChE and MAO-B inhibitor with IC50 values of 1.72 μM and 0.950 μM against AChE and MAO-B, respectively. K2V-9 inhibits amyloid β self-aggregation and reduces ROS. K2V-9 has neuroprotective effects.

RDS-04-010 is an atypical dopamine transporter (DAT) inhibitor. RDS-04-010 has the effect of inhibiting cocaine intake and seeking behavior. RDS-04-010 exerts its modulatory effect mainly by binding to the inward conformation of DAT, thereby reducing the reinforcing effect of cocaine. RDS-04-010 can be used in the study of cocaine use disorder (CUD).

Naperiglipron (LY3549492) (Example 2) is a Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC50 of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC50: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research.

Photosensitizer-7 is a endoplasmic reticulum (ER)-targeted photosensitizer (PS) (λab = 610 nm, λem = 622 nm). Photosensitizer-7shows an IC50 of 4.006 μM in HeLa cells and 3.28 μM in MCF-7 cells under light irradiation. Photosensitizer-7 exhibits dose-dependent cellular uptake and predominant colocalization with ER. Photosensitizer-7 induces dose-dependent intracellular ROS generation, reduces mitochondrial membrane potential, and increases apoptosis upon light irradiation in cells. Photosensitizer-7 significantly inhibits tumor growth in MCF-7 tumor-bearing mice. Photosensitizer-7 can be used for the study of photodynamic anticancer applications.

A-228839 is a potent farnesyltransferase inhibitor. A-228839 inhibits lymphocyte activation and cytokine production.

TRK-530 sodium is an orally active bisphosphonate. TRK-530 sodium inhibits CINC-1. TRK-530 sodium inhibits dental calculus formation. TRK-530 sodium also inhibits paw edema, joint destruction and osteomyelitis.

Alanycarb (OK-135) is a broad-spectrum oxime carbamate insecticide with contact and oral toxicity. Alanycarb is effective against a wide variety of insect pests and is a pro-insecticide. The principal active molecule produced by the biological modification of Alanycarb within target organisms is methomyl.

T 162559 is a potent and selective inhibitor of the Na+/H+ exchanger isoform NHE1 with IC50 values of 0.96 nM. T 162559 does not affect Na+/HCO3- cotransport and Na+/Ca2+ exchange. T 162559 can be used for the research of cardiovascular disease.

(R)-Pirlindole mesylate is selective and reversible a Monoamine oxidase A (MAO-A) inhibitor with an IC50 of 0.43  μM for MAO-A over MAO-B. (R)-Pirlindole mesylate has an antidepressant activity. (R)-Pirlindole mesylate significantly decreases immobility time of the forced swim test and inhibits Reserpine-induced palpebral ptosis in behavioural mice models. (R)-Pirlindole mesylate can be used for depression research.

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).

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.

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.

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.

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.

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.

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).

(Z)-1,2-Dimethoxy-4-(3-fluoro-2-propenyl)benzene is a fluorine analog of Methyl eugenol (ME) and is attractive to oriental fruit fly B. dorsalis.

BRP-821 is a soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 0.4 nM. BRP-821 can be used for the researches of inflammation, cardiovascular, metabolic and neurological disease .

AR-DBD ligand-Linker Conjugate 1 is a conjugate of AR-DBD ligand and linker. AR-DBD ligand-Linker Conjugate 1 can be used to synthesize PROTAC LYA914.

TBS6b is a potent and selective ACKR3 molecular glue degrader. TBS6b degrades ACKR3 via the ubiquitin-proteasome pathway. TBS6b inhibits hepatocellular carcinoma cell proliferation, migration, and invasion. TBS6b is relevant to hepatocellular carcinoma (HCC) research.