Isotope-Labeled Polyketides

Genistein-d₄ is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.

Cyclosporin A-d₄ (Cyclosporine A-d₄) is the deuterated-labeled Cyclosporin A (HY-B0579). Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

Daidzein-d₄ is the deuterium labeled Daidzein. Daidzein is a soy isoflavone, which acts as a PPAR activator.

Clarithromycin-¹³C,d₃ is the deuterium and ¹³C labeled Clarithromycin.

Tacrolimus-¹³C,d₂ (FK506-¹³C,d₂) is the ¹³C, deuterated-labeled Tacrolimus (HY-13756). Tacrolimus (FK506), a molecular glue, a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.

Daunorubicin-¹³C,d₃ TFA (Daunomycin-¹³C,d₃ TFA) is the deuterium and ¹³C-labeled Daunorubicin TFA. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.

Liquiritigenin-d₄ (4',7-Dihydroxyflavanone-d₄) is the deuterium labeled Liquiritigenin (HY-N0377). Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC₅₀ of 36.5 nM for activation of the ERE tk-Luc.

α-Zearalenol-¹³C₁₈ is the ¹³C-labeled α-Zearalenol. α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER). α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects.

Naringenin-d₄ is the deuterated version of Naringenin (HY-N0100). Naringenin shows strong anti-inflammatory and antioxidant activities. Naringenin has anti-dengue virus (DENV) activity.

(±)-Equol-d₄ is the deuterium labeled (±)-Equol.

Resveratrol-d₄ is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.

Azithromycin-d₃ is the deuterium labeled Azithromycin. Azithromycin (CP-62993) is a macrolide antibiotic useful for the treatment of a number of bacterial infections.

Quercetin-d₃ is the deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC₅₀ of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Rapamycin-d₃ (Sirolimus-d_{3; AY-22989-d3; NSC 226080-d3}) is the deuterated-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.

Clarithromycin-d₃ is the deuterium labeled Clarithromycin (HY-17508). Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.

Doxorubicin-¹³C,d₃ TFA is the deuterium and ¹³C labeled Doxorubicin. Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stoppin

Zearalenone-¹³C₁₈ (Mycotoxin F2-¹³C₁₈; Toxin F2-¹³C₁₈) is the ¹³C labeled Zearalenone (HY-103447). Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts.

Apigenin-d5 is a deuterated labeled Apigenin. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a K_i of 2 μM.

Erythromycin-¹³C,d₃ is the ¹³C- and deuterium labeled Erythromycin. Erythromycin is a macrolide antibiotic produced by actinomycete?Streptomyces erythreus?with a broad spectrum of antimicrobial activity. Erythromycin acts by binding to bacterial 50S ribosomal subunits and inhibits?RNA-dependent protein synthesis?by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid.

Rapamycin-¹³C,d₃ (Sirolimus-¹³C,d₃) is the ¹³C, deuterated-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.