macrocyclic

Oenothein B is a specific inhibitor of poly(ADP-ribose) glycohydrolase. Oenothein B shows antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties.

Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid extracted from the seeds of Crotalaria plants. It inhibits organic cation transporters OCT-1 and OCT-2, with IC50 values of 36.8 µM and 1.8 mM, respectively. Monocrotaline exhibits antitumor activity and shows certain cytotoxicity against liver cancer cells such as HepG2. It is also commonly used to induce pulmonary arterial hypertension models in rodents.

Selamectin (UK-124114) is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. In an H. contortus larval development assay, selamectin (0.1 μg/ml) shows the effect of growth inhibition.

Methyl-β-cyclodextrin (Methyl-beta-cyclodextrin) is a macrocyclic compound utilized as a solubilizer for hydrophobic substances in biological studies, and serves as a lipid raft inhibitor with cholesterol-lowering and potential antitumor activities.

Spinosad is a naturally-occurring insecticide found in the the soil bacterium S. spinosa. It is a mixture of the macrocyclic lactones spinosyn A and spinosyn D, which act as agonists of insect nicotinic acetylcholinesterase receptors (nAChRs).

ω-Pentadecalactone (Exaltolide) is the fragrance structural group macrocyclic lactone and lactide derivatives used as a fragrance ingredient.

UK-124114 (Selamectin) is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. In an H. contortus larval development assay, selamectin (0.1 μg/ml) shows the effect of growth inhibition.

Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay).

Micrococcin P1 is a macrocyclic peptide antibiotic and a potent inhibitor of the hepatitis C virus (HCV) with an EC50 range of 0.1-0.5 μM.

Virginiamycin M1 (Pristinamycin IIA) is a macrocyclic lactone peptide antibiotic and is a member of the streptogramin A group of antibiotics.

Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by *Streptomyces actuosus*, is a potent feed additive that promotes animal growth by inhibiting bacterial protein synthesis. It is characterized by an indole side ring system and regiospecific hydroxyl groups on its macrocyclic core.

2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) is a macrocyclic DOTA derivative developed for tumor pretargeting.

AZD5991 is a potent and selective Mcl-1 inhibitor aimed at treating hematological cancers. As a well-designed macrocyclic compound, AZD5991 exhibits sub-nanomolar affinity for Mcl-1. It primarily inhibits the myeloid cell leukemia-1 protein (Mcl-1; Bcl2-L-3), showing potential pro-apoptotic and anti-tumor activity. AZD5991 binds to Mcl-1, preventing its interaction with certain pro-apoptotic proteins, leading to apoptosis in cells overexpressing Mcl-1.

UNC8969 is a macrocyclic dual MERTK/AXL inhibitor (IC50 MERTK = 1.1 nM; IC50 AXL = 5.3 nM). The compound exhibits low nanomolar activity against MERTK and AXL while demonstrating good selectivity over TYRO3 and FLT3. Target binding and selectivity have been confirmed through NanoBRET and cell-based MERTK and AXL phosphorylation assays. UNC8969 possesses excellent pharmacokinetic properties (large AUC and long half-life) and shows exceptional anti-tumor activity against lung cancer cell lines, indicating its potential as a therapeutic compound.

Megalomicin is a macrocyclic lactone antibiotic complex produced by Micromonospora.

HDAC11-IN-1 (Compound 14-NC6OH) is a macrocyclic inhibitor that selectively targets HDAC11 with a Ki of 40 nM. It demonstrates effective cell permeability and suppresses the expression of YAP1 and SOX2.

p-SCN-Bn-NOTA is a stable and highly affinity integrator. It is a compound with a macrocyclic structure, consisting of two parts: SCN and Bn NOTA. Among them, SCN has the ability to chelate metal ions. This dual-functional group can simultaneously bind to metal ions and biological molecules, achieving specific biological goals.

BMS-986238 is a second-generation macrocyclic peptide and an effective PD-L1 inhibitor. It holds potential for research in the treatment of solid tumors and lymphomas (cancer of the lymphatic system).

Zosurabalpin TFA is a macrocyclic peptide antibiotic that specifically targets Acinetobacter baumannii (A. baumannii) by inhibiting lipopolysaccharide transport.

20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the 20S proteasome, with IC50 values of 0.19 μM for chymotrypsin-like (ChT-L) activity and 52.5 μM for peptidylglutamyl-peptide hydrolyzing-like (PGPH-L) activity.

HDAC11-IN-1 (Compound 14-NC6OH) TFA is a selective macrocyclic inhibitor of HDAC11, with a Ki of 40 nM. It possesses excellent cell permeability and is capable of inhibiting the expression of YAP1 and SOX2.

TAM-IN-1 (compound 1) is a potent macrocyclic inhibitor targeting Axl and Mer, with Ki values of 130 pM and <50 pM, respectively.

CID-078 is an oral macrocyclic cyclin A/B-RxL dual inhibitor. CID-078 binds to the hydrophobic patch region of Cyclin A/B, disrupting protein-protein interactions within the HP-RxL-mediated Cyclin A2/CDK2–E2F1 and Cyclin B1/CDK1–MYT1 complexes, leading to cell cycle arrest and tumor apoptosis. CID-078 selectively kills E2F pathway-driven tumor cells and induces tumor regression in mouse xenograft models. CID-078 is suitable for research on advanced solid tumors, including small cell lung cancer, triple-negative breast cancer, neuroendocrine cancer, and CDK4/6 inhibitor-resistant breast cancer.

Janthinocin A is a macrocyclic peptide lactone antibiotic.