CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein)[1].
ATR-IN-24 (Compound 1) is a ATR inhibitor. ATR-IN-24 has anticancer activity[1].
Podocarpusflavone A is a DNA topoisomerase I inhibitor, have moderated anti-proliferative activity induce cell apoptosis in MCF-7, is developing anti-tumor drugstarget: DNA topoisomerase IIn vitro: podocarpusflavone-A show significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines (ED50 4.56-16.24 μg/mL) and induce cell apoptosis in MCF-7 via mainly sub-G1/S phase arrest. PF (40 ug/mL, 24 hr) significantly induced about 10 folds of cell deaths and growth arrest in S-phase than the control group.
3’-Azido-N6-benzoyl-3’-deoxyadenosine 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].
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models[1].
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM)[1][2]. PIK-75 induces apoptosis[3].
Antibacterial agent 124 (Compound 3) is a potent bacterial prolyl-tRNA synthetase (ProRS) inhibitor with an IC50 of 0.18 μM against Staphylococcus aureus ProRS (SaProRS)[1].
3’-O-MOE-G(iBu)-2’-phosphoramidite is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
5-Hydroxymethyl xylouridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
2'-O-MOE-rC is a 2'-O-MOE modified nucleoside. 2'-O-MOE-rC can be used for synthesis of DNA[1][2].
1-(β-D-Xylofuranosyl)-5-methyluracil is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Deoxycytidine triphosphate (dCTP), a nucleoside triphosphate, is a raw material in DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle[1].
2’-Bromo-2’-deoxy-5-methyluridine 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].
8-Azaguanine is a purine analogue which shows antineoplastic activity.
Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.
8-Methoxyadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively[1].
Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability[1].
UIAA-II-232 (compound 19b) is a potent DNA gyrase catalytic inhibitor with an IC50 value of 3.5 µM[1].
5-(Trifluoromethyl)cytidine 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].
Mps-BAY2a is a monopolar spindle 1 (MPS1) inhibitor with an IC50 of 1 nM against human MPS1. Mps-BAY2a induces mitotic aberrations and apoptosis in cancer cells[1].
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research[1].
Rivoglitazone is a thiazolidinedione-derivative PPARγ agonist for the treatment of type 2 diabetes mellitus.
2-Chloro-2'-deoxy-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia[1][2].
Antibacterial agent 89 is a potent antibacterial agent. Antibacterial agent 89 shows anti-clostridial activity. Antibacterial agent 89 inhibits the release of cytotoxins and the β’CH-σ interaction. Antibacterial agent 89 disrupts the process of bacterial transcription[1].
2’-Amino-2’-deoxy-β-D-arabino-5-methyl uridine 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].
4-Deoxy-xylo-uridine 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].
MC-betaglucuronide-MMAE-1 is a drug-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
6-Thioguanosine (6-Mercaptoguanosine), an active nucleoside, is an Azathioprine metabolite. 6-Thioguanosine has immunosuppressive effects[1].