TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively.

PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats.

Pomalidomide-5-OH (5-hydroxy pomalidomide) is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTAC.

Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis.

Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood.

Thalidomide-Piperazine-PEG1-NH2 diTFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

FPI-1523, a derivative of Avibactam, is a potent β-lactamase inhibitor, with Kds of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively. FPI-1523 also inhibits PBP2, with an IC50 of 3.2 μM. FPI-1523 exhibits considerable antimicrobial activity.

FPI-1523 sodium, a derivative of Avibactam, is a potent β-lactamase inhibitor, with Kds of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively. FPI-1523 sodium also inhibits PBP2, with an IC50 of 3.2 μM. FPI-1523 sodium exhibits considerable antimicrobial activity.

Irsenontrine (E2027) is an orally active and selective phosphodiesterase 9 (PDE 9) inhibitor. Irsenontrine can be used for the research of neurological diseases.

BN82002 hydrochloride is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 hydrochloride inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 hydrochloride displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.

Salsolidine hydrochloride, a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A (monoamine oxidase A) inhibitor.

IHVR-11029 is a small molecule inhibitor of ER α-glucosidases, with an EC50 of 0.09 μM.

Violanone, an isoflavanone compound, can inhibit tubulin polymerization. Violanone also exhibits larvicidal activity against A. aegypti.

UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research.

OICR-9429-N-C2-NH2 is a ligand for Wd40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1, intermediate 2. OICR-9429-N-C2-NH2 can be used in the synthesis of PROTACs.

RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM.

STK33-IN-1 (compound 1) is a STK33 inhibitor, with an IC50 of 7 nM.

Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion.

Ruzinurad is a highly selective URATl inhibitor (WO2020088641, compound I). Ruzinurad can be used in the study of hyperuricemia.

Idrevloride, an epithelial sodium channel (ENaC) inhibitor (WO2016133967), can be used for the research of skin disorders.

Iedaborbactam, as a beta-lactamase inhibitor (WO2015191907, Example 62), can be used for the research of bacterial infections.

MAT2A inhibitor 4 is an inhibitor of the catalytic subunit of methionine S-adenosyltransferase-2 (MAT2A). MAT2A inhibitor 4 can be used for the research of cancer.

Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can attenuate cocaine-induced locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer.

Aganepag isopropyl (AGN-210961) is an EP2 agonist.

Tilpisertib is a serine/threonine kinase inhibitor (WO2017007689).

MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.

IACS-8803 diammonium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 diammonium has a robust systemic antitumor efficacy.

Tyrosylleucine (Tyr-Leu, YL), an orally active dipeptide, exhibits a potent antidepressant-like activity.

Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency.

Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects.