Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential[1].
DNA-PK-IN-10 is a DNA-PK inhibitor. DNA-PK-IN-10 can be used for the research of breast cancer and non-small cell lung cancer[1].
AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
Rubitecan (RFS 2000), a camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells[1][2][3].
Nicotinamide riboside malate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities[1]. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease[2].
Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
Vinflunine is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.Target: Microtubule/TubulinThe major effects of Vinflunine on dynamic instability are a slowing of the microtubule growth rate, an increase in growth duration, and a reduction in shortening duration. The effects of Vinflunine on the readmilling rate is examined by following [3H]GTP incorporation into MAP-rich microtubules, and the IC50 is 0.42 μM [1]. Vinflunine induced mitotic accumulation with IC50 with 18.8 nM, which decreases the centromere dynamicity by 44% and increases the time centromeres spent ina paused state by 63% [2]. Treatment of Vinflunine induces a rapid change in endothelial cell shape: cells retracts and assumes a rounded morphology. Mean IC50 values are 9.9 × 10-5 M × 10-5 M for fibronectin and 5.0× 10-5 M × 10-5 M for type IV collagen. A short 4 hours exposure of endothelial cells to Vinflunine at 10-8 0.05). An ID50 value (dose which inhibits 50% of bFGF-induced neovascularisation) is calculated as 1 mg/kg. Low doses of Vinflunine reduce the number of experimental liver metastases by human LS174T colon cancer cell. A slight overall decrease in liver metastatic foci is already observed at the very low dose of 0.16 mg/kg Vinflunine, although maximal overall inhibition is reached at the maximal tolerated dose (MTD) of 20 mg/kg [3].
Brefeldin A is a specific inhibitor of protein trafficking which blocks the protein transport from the endoplasmic reticulum to the Golgi complex.
Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases[1].
ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively[1].
IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
Nalidixic Acid-d5 is the deuterium labeled Nalidixic acid. Nalidixic acid, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria[1].
Sorivudine (BV-araU) is an orally active synthetic pyrimidine nucleoside antimetabolite drug. Sorivudine derives its antiviral activity from selective conversion by a specific thymidine kinase present in certain DNA viruses to nucleotides, which can in turn interfere with viral DNA synthesis[1].
SRT 1720 Hydrochloride is a selective activator of SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities on SIRT2 and SIRT3 with EC1.5s of 37 μM and 300 μM, respectively.
CHIC35, an analog of EX-527, is a potent and selective inhibitor of SIRT1 (IC50=0.124 µM). CHIC35 shows potential selective inhibition against SIRT1 over SIRT2 (IC50=2.8 µM) or SIRT3 (IC50>100 µM)[1]. CHIC35 has anti-inflammatory effects and can be used for CHARGE syndrome research[1][2].
5-Methylcytidine 5′-triphosphate (5-Methyl-CTP) is a modified nucleoside triphosphates. 5-Methylcytidine 5′-triphosphate can apply in replacing unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells[1].
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells[1].
2'-F-Bz-dC Phosphoramidite can be used in the synthesis of oligoribonucleotides[1].
Thymidine-13C-1 is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1].
8-Benzyloxy-3’-deoxy-3’-fluoroguanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Remdesivir is a nucleoside analogue, with effective antiviral activity, with EC50s of 74 nM for ARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells.
6-Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα[1][2].
NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
N-Trityl-morpholino-T-5'-O-phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
DENV-IN-5 (Compound 4b) is a dengue virus (DENV) inhibitor with EC50s of 1.47, 9.23, 7.08 and 8.91 μM against DENV-I ∼ IV replication, respectively. DENV-IN-5 also inhibits HIV-1IIIB strain with an EC50 of 0.1512 μM[1].
AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively[1][2].
1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells[1].
3’-Deoxy-3’-α-C-methyl-N6,N6-dimethyladenosine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
2-Methyladenosine is an adenosine analogue. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. The popular products in this series are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].