Metabolism

NADH-IN-2 (compound 8) is a Type II NADH dehydrogenase inhibitor.

Docosapentaenoic acid (22n-3) sodium is a component of phospholipids. It exhibits inhibitory activity against α-amylase and α-glucosidase, with IC50 values of 17 μg/mL and 22 μg/mL, respectively. Additionally, Docosapentaenoic acid 22n-3 sodium enhances cell viability and has mild anti-inflammatory effects.

RORγt inhibitor 4 (Compound 9a) is an orally active RORγt inhibitor capable of penetrating the central nervous system. It has been shown to improve experimental autoimmune encephalomyelitis.

DLCI-1 is a potent and selective oral inhibitor of cytochrome P450 2A6 (CYP2A6), significantly reducing self-administered nicotine doses in both male and female mice.

Cephapirinlactone is a metabolite of the antibiotic Cephapirin.

Indoluidin E selectively inhibits DHODH and has an inhibitory effect on cancer cell growth.

Lipid PPz-2R1 is an ionizable cationic lipid employed in crafting lipid nanoparticles (LNPs) for mRNA delivery both in vitro and in vivo. LNPs with lipid PPz-2R1, encapsulating an mRNA reporter, target the lungs preferentially over the heart, liver, spleen, and kidneys in mice. Additionally, these LNPs, when encapsulating mRNA encoding phosphatase and tensin homolog (PTEN), enhance PTEN protein levels in PTEN-deficient Lewis lung carcinoma (LLC) cells. In an orthotopic murine LLC model, these Lipid PPz-2R1-containing LNPs, carrying PTEN mRNA, reduce tumor growth either when administered alone or alongside an antibody against programmed cell death protein 1 (PD-1).

ABT-046 is an orally active, selective, and highly efficient Diacylglycerol Acyltransferase 1 (DGAT-1) inhibitor that can be used in metabolic disease research.

Complex III-IN-2 inhibits complex III, with antifungal EC50: 29.31 mg/L vs R. solani, 29.98 mg/L vs S. sclerotiorum.

orally active ghrelin receptor (GHS-R1a) agonist

RXR antagonist 2 is a potent antagonist of RXR (Ki: 0.391 μM, Kd: 0.281 μM). RXR antagonist 2 has shown research potential for RXR-related diseases.

Nampt-IN-13 (example 58m) is an NAMPT inhibitor used in the synthesis of antibody-drug conjugates (ADCs).

Canosimibe is a cholesterol absorption inhibitor

Nampt-IN-14 (example 3) is an effective NAMPT inhibitor with an IC50 of 0.2 nM, suited for use in the synthesis of antibody-drug conjugates (ADCs).

ONL-1204 is a small molecule, CD95 antigen inhibitor (Fas inhibitor) being developed by ONL Therapeutics for the treatment of retinal detachment.

Ranolisib is an isocitrate dehydrogenase (IDH) inhibitor known for its antitumor activity.

ABCB1-IN-4 (Compound C6z) is an orally active inhibitor of α-amylase and α-glucosidase, with IC50 values of 1.63 μM and 0.14 μM, respectively. It holds potential for diabetes research.

Pyripyropene A is a potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2)(IC50 of 0.07 μM).

Potent hCA inhibitor: targets hCA II, IX & XII with IC50s of 42.9, 47.6, & 6.7 nM respectively.

NTPDase-IN-1 selectively inhibits NTPDases 1, 2, 8 with IC50 of 0.05, 0.23, 0.54 μM. Non-competitive, K m 21 μM, used in cancer, immune, infection research.