Metabolism

CA inhibitor 4, photoprobe; targets hCA I-XIV; Ki: 640-1166 nM.

PHGDH-IN-2: potent PHGDH inhibitor, IC50=5.2μM; hinders PHGDH cancer cell growth & serine synthesis in MDA-MB-468.

(±)-HIP-B is an excitatory amino acid transporter blocker.

Compound B15: potent sEH inhibitor (0.03 nm), reduces inflammation & pain.

Nampt-IN-15 (Example 3) is a Nampt inhibitor that exhibits cytotoxic effects on various cell lines, including BxPC-3, HepG2, L540cy, and MOLM-13. The respective IC50 values for these cell lines are 38.5 nM, 8 nM, 8.5 nM, and 7 nM.

Lp(a)-IN-7 (example 1) is an inhibitor of lipoprotein (a) [Lp(a)] formation, exhibiting an IC50 of 2.51 nM in media containing apolipoprotein B (apoB) and apolipoprotein (a). This compound is applicable in cardiovascular disease research.

SHP2 IN-1 is an allergic SHP2 (PTPN11) inhibitor(IC50 : 3 nM).

RORγt inverse agonist 32 (compound b14) exhibits oral activity and can be utilized in inflammatory research studies.

Beloranib is a fumagillin anticancer drug. Beloranib belongs to an angiogenesis inhibitor.

Carbonic anhydrase inhibitor 3 (compound 11g) is an inhibitor of carbonic anhydrase II that reduces the intraocular pressure in glaucomatous rabbits [1].

PENAO is a potent mitochondrial toxin for tumor cells. It deactivates the mitochondria of tumor cells by targeting the adenine nucleotide translocase in the cell membrane.

Enpp-1-IN-7: potent enpp-1 inhibitor, broad specificity, potential in cancer/infectious disease research. (WO2021203772A1)

1-Stearoyl-sn-glycerol 3-phosphate sodium, a biologically active phospholipid, plays a crucial role in regulating cell motility, proliferation, invasion, survival, and the production of growth factors through interactions with G protein-coupled receptors (GPCR). Synthesized during the formation of membrane phospholipids, this compound typically has a low plasma concentration (approximately 100nM) and originates from various cell types, including activated platelets, epithelial cells, leukocytes, neuronal cells, and tumor cells. Its distinctive structure features stearic acid at the sn-1 position and a hydroxyl group at the sn-2 position.

RMGPa-IN-1 (Compound 10C) is an inhibitor of rabbit muscle glycogen phosphorylase a (RMGPa), exhibiting an IC50 value of 82.5 μM. This compound holds potential for research in diabetes.

DOCP (2-((2,3-Bis(oleoyloxy)propyl)dimethylammonio)ethyl hydrogen phosphate) is a lipid characterized by an opposite charge orientation compared to traditional phosphatidylcholine (PC) lipids, featuring quaternary ammonium near the bilayer interface and phosphate groups projecting into the aqueous environment. This unique structure of iPC lipids presents an excellent opportunity to investigate the biophysical characteristics and biological activities influenced by the reversal of surface charges on bilayers.

α-Glucosidase-IN-17 (Compound 12B) is a potent and orally active inhibitor of α-glucosidase, demonstrating antidiabetic activity with an inhibitory

Diacylglycerol Acyltransferase Inhibitor-1, a diacylglycerol acyltransferase (DGAT1) inhibitor, effectively suppresses the activity of DGAT1.

FXIa-6f is a high affinity, orally bioavailable macrocyclic FXIa inhibitor with antithrombotic activity in preclinical species

FXR/HSD17B13 modulator 1 (compound 6) is an effective modulator of FXR/HSD17B13, playing a significant role in studies related to metabolic dysfunction-associated steatohepatitis (MASH).

OSI-413 (free base) (CP 373413) is the primary metabolite of Erlotinib. Erlotinib (CP-358774) acts as a direct EGFR tyrosine kinase inhibitor with an IC50 of 2 nM against human EGFR.