3’-β-C-Ethynylguanosine 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].
2’-Bromo-2’-deoxy-5-fluorouridine 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].
Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12[1].
HDAC ligand-1 is a HDAC ligand that can be used to synthesize PROTAC HDAC degraders[1].
N2-iso-Butyroyl-5'-O-DMT-3'-deoxy-3'-fluoroguanosine 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-Pyrrolidinomethyluridine 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].
Tubulin polymerization-IN-36 is a tubulin polymerization inhibitor (IC50: 2.8 μΜ). Tubulin polymerization-IN-36 binds to the colchicine site of tubulin and inhibits colchicine binding. Tubulin polymerization-IN-36 can be used in the research of cancers, such as lymphomas[1].
Among vibsanin a analogues, vibsanin a analog C (VAC) showed anti proliferative effect on various cancer cell lines, and the anti proliferative activity was the strongest among vibsanin a analogues. In addition, VAC fluctuated the amount of hsp90 related proteins in cells and inhibited hsp90 mediated protein refolding of luciferase in vitro.
Bocodepsin (OKI-179) is an orally active and selective HDAC inhibitor, with antitumor activity. Bocodepsin can be used for suppression on solid tumor and hematologic malignancies[1].
Tibremciclib is a CDK4 inhibitor with antineoplastic activity[1].
Sipoglitazar is an orally active agonist of PPAR. Sipoglitazar can be used to study diabetes[1].
Hsp90-IN-17 (Example 5) hydrochloride is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases[1].
CDK-IN-12 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC50 values less than 20 nM[1].
1,N6-Etheno-ara-adenosine 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].
Tenacigenin B is a steroid that can be isolated from the genus Alocasia. Tenacigenin B has anti-tumor effects on lymphoma via regulation of Aurora-A[1][2].
SPHINX31 is a potent and selective inhibitor of serine/arginine-rich protein kinase 1 (SRPK1), with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1), which is a SRPK1 substrate. SPHINX31 is a potential topical therapeutic for neovascular eye disease[1].
5′-Azido-5′-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].
Alyssin, found in Cruciferous Vegetables, exerts anticancer activity in HepG2 by increasing intracellular reactive oxygen species and tubulin depolymerization[1].
GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin[1].
XAV-939 is a tankyrase (TNKS) inhibitor and an indirect inhibitor of Wnt/β-catenin signaling, with IC50s of 5 and 2 nM for TNKS1 and TNKS2, respectively.
Guanine is one of the fundamental components of nucleic acids (DNA and RNA). Guanine is a purine derivative, consisting of a fused pyrimidine-imidazole ring system with conjugated double bonds.
Triclabendazole(CGA89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.Target: Microtubule/TubulinTriclabendazole treatment produces percentage decreases of the fluke egg output by 15.3%, 4.3% and 36.6%, respectively, in sheep, dairy cows and heifers, these results indicate the presence of TCBZ-resistant Fasciola hepatica in sheep and cattle on this farm [1]. Triclabendazole sulphoxide (50 mg/mL) results in extensive damage to the tegument of triclabendazole-susceptible F. hepatica, whereas triclabendazole-resistant flukes shows only localized and relatively minor disruption of the tegument covering the spines [2].Triclabendazole is metabolized into a number of compounds, depending on the route of administration, plasma levels peak at 18-24 hours (Triclabendazole sulphoxide) and 36-48 hours (Triclabendazole sulphone), neither Triclabendazole nor any toher metabolites can be detected in plasma. Triclabendazole sulphoxide blocks the transport of secretory bodies from the cell body to the tegumental surface, the block occurs at the site of their formation by the Golgi complex in the cell body, in their movement through the cytoplasmic connections to the syncytium, and in their movement from the base to the apex of the syncytium. Triclabendazole binds to the colchicine binding site on the β-tubulin molecule and this has been used at the basis for evaluating the relative acitvity of Triclabendazole [3].
Neoxanthin is a major xanthophyll carotenoid and a precursor of the plant hormone abscisic acid in dark green leafy vegetables. Neoxanthin is a potent antioxidant and light-harvesting pigment. Neoxanthin induces apoptosis and has anticancer actions[1][2].
2’-Fluoro-2’-deoxy-N6-methylarabinoadenosine 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].
N-Propargyladenosine 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].
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis[1].
Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of cisplatin and a potent anti-cancer agent.
5'-O-TBDMS-dG is a modified nucleoside. 5'-O-DMT-2'-O-TBDMS-rI can be used in the synthesis of deoxyribonucleic acid or nucleic acid.
3’-Azido-3’-deoxycytidine 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].
CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC50: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560)[1].