3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid is a target protein ligand-linker conjugate that incorporates a ligand for c-Met and a PROTAC linker, which recruits E3 ligases. 3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid can be used in the synthesis of PROTACs, such as SJF-8240

KIN-8741 is a highly selective Type IIb c-Met inhibitor. KIN-8741 has broad activity against c-Met kinase mutations. KIN-8741 shows antitumor activity in MET gene amplified and exon 14 deleted non-small cell lung cancer models. KIN-8741 can be used in the research of c-Met driven cancers, especially advanced tumors carrying MET exon 14 jump mutations, acquired drug resistance mutations, etc.

Anion transporter-4 (Compound 6) is a small-molecule anion transporter, which induces tubulin degradation and mitochondrial dysfunction. Anion transporter-4 can increase intracellular anion levels such as chloride ions by disrupting microtubule dynamics, promoting lipid peroxidation, and impairing mitochondrial function. Anion transporter-4 triggers ferroptosis to exert anticancer activity. Anion transporter-4 is promising for research of cancers.

OX2-2303 is a potent, selective orexin-2 receptor (OX2R) antagonist. OX2-2303 exhibits excellent binding affinity towards OX2R (Ki = 0.1 nM), and shows >890-fold selectivity over OX1R. OX2-2303 can be used as a positron emission tomography (PET) radioligand for central nervous system (CNS) research.

ELQ-453 is an inhibitor targeting the Qo site of the Plasmodium falciparum cytochrome bc1 complex (CytB) with an IC50 value of 0.57 nM. ELQ-453 blocks the mitochondrial function of the parasite, and suppresses Plasmodium infection in mosquitoes. ELQ-453 is promising for research of malaria.

AZD3839 (fumarate) is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 (fumarate) inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 (fumarate) inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 (fumarate) binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 (fumarate) can be used in the field of Alzheimer's disease research.

LP-65 is a dual inhibitor of MEK (IC50=83.2 nM) and mTOR (IC50=40.5 nM). LP-65 blocks MEK and mTOR signaling pathways and inhibits tumor cell proliferation and migration. LP-65 is promising for research of cancers.

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.

CP-800569 is an orally active cholesteryl ester transfer protein (CETP) inhibitor. CP-800569 can decrease low-density lipoprotein and postprandial triglyceride and increase high-density lipoprotein. CP-800569 can be used for the research of metabolic disease.

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.