RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a cytidine analog; shows anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.IC50 value: 0.4- >30 nM (15 cancer cell lines) [1]Target: cytidine analogin vitro: RX-3117 showed a different sensitivity profile compared to cyclopentenyl-cytosine (CPEC) and azacytidine, substrates for uridine-cytidine-kinase (UCK).RX-3117 was a very poor substrate for cytidine deaminase (66,000-fold less than gemcitabine). In sensitive U937 cells 1 μM RX-3117 resulted in 90% inhibition of RNA synthesis but 100 μM RX-3117 was required in A2780 and CCRF-CEM cells. RX-3117 at IC50 values did not affect the integrity of RNA [1].in vivo: Orally-administered RX-3117 was examined in 9 different human tumor xenograft models (colon, non-small cell lung, small cell lung, pancreatic, renal and cervical), grown subcutaneously in athymic nude mice. In the Colo 205, H460, H69 and CaSki models, gemcitabine treatment resulted in 28%, 30%, 25% and 0% tumor growth inhibition (TGI), respectively, whereas oral treatment with RX-3117 induced 100%, 78%, 62% and 66% TGI, respectively [2].
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP.
Bocodepsin hydrochloride (OKI-179) is an orally active and selective HDAC inhibitor, with antitumor activity. Bocodepsin hydrochloride can be used for suppression on solid tumor and hematologic malignancies[1].
4-Deoxy-3’-β-C-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].
OTS-964 is a potent TOPK inhibitor (IC50=28 nM), which inhibits TOPK kinase activity with high affinity and selectivity.
Epothilone E is a related compound of epothilone, which inhibits microtubule protein function and blocks cell division, and has anti-tumor activity[1].
CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively[1].
5’-Azido-5’-deoxy-2’-O-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].
HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82, 45, and 24 nM, respectively. HDAC-IN-43 is a weak PI3K/mTOR inhibitors with IC50 values of 3.6 and 3.7 μM, respectively. HDAC-IN-43 shows broad anti-proliferative activity [1].
3′-Deoxy-3′-fluorouridine 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].
PPARγ agonist 5 (Compound 1) is a potent and selective agonist of PPARγ. PPARγ agonist 5 has the potential for the research of cancer diseases[1].
Panobinostat is a non-selective histone deacetylase (HDAC) inhibitor.
KD3010 is a potent, orally active, and selective PPARδ agonist.
3’-Azido-3’-deoxy-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].
PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively.
5-Fluoro-4’-thiouridine 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].
KU 59403 is a potent ATM inhibitor, with an IC50 of 3 nM.
Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle[1]. Antitumor activity[2].
Adenosine-13C5 is the 13C labeled Adenosine[1]. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[2][3].
CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC50 of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects[1].
Thio-ITP (6-Thioinosine 5′-triphosphate) is a RNA polymerase activities competitive inhibitor[1].
N6-Benzoyl-3'-fluoro-2',3'-dideoxyadenosine 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].
2-Aminofluorene is a synthetic chemical insecticide. 2-Aminofluorene is a genotoxin. 2-Aminofluorene can be used in the research of DNA adduct structure, DNA repair, carcinogenesis, and mutagenesis[1][4].
NRD167 is a potent and selective SIRT5 inhibitor.
Dihydrodeoxyuridine (H2dUrd) 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].
N-Nitrosodiethylamine-d4 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
HA15-Biotin is a chemical probe that consists of HA15 and biotin attached on the amide part of HA15. HA15-Biotin exhibits similar levels of activity to HA15. HA15-Biotin can be used for proteomic analysis[1].
PERK-IN-3 is a potent PERK inhibitor with an IC50 of 7.4 nM[1].
WEHI-150 is a replica of mitoxantrone, is a portent DNA interstrand crosslink[1].
Tipiracil is a thymidine phosphorylase (TPase) inhibitor.