Angeloylgomisin H, as a major lignin extract of Schisandra rubriflora, has the potential to improve insulin-stimulated glucose uptake by activating PPAR-γ[1].
Tenovin-6 is a water soluble inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively.
9-((2R,3R,4R,5R)-4-Hydroxy-5-(hydroxymethyl)-3-methoxytetrahydrofuran-2-yl)-9H-purin-6-ol (2'-O-methylinosine) 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].
eIF4A3-IN-8 is a selective ATP-competitive eukaryotic initiation factor 4A3 (eIF4A3) inhibitor. eIF4A3-IN-8 can serve as a valuable chemical probe to elucidate the detailed function of eIF4A3 and EJC (exon junction complex)[1].
DMT-dG(dmf) Phosphoramidite is a phosphinamide monomer that can be used in the preparation of oligonucleotides
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].
RNA splicing modulator 2 (compound 256) is a RNA splicing modulator[1].
Nicotinamide riboside chloride is a crystal form of Nicotinamide riboside (NR) chloride which is a nicotinamide adenine dinucleotide (NAD[+]) precursor vitamin. Nicotinamide riboside chloride increases NAD[+] levels and activates SIRT1 and SIRT3, culminating in enhanced oxidative metabolism and protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside chloride is used in dietary supplements[1].
ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
4’-C-Methyl-5-methylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Alvespimycin hydrochloride is a potent inhibitor of Hsp90, binding to Hsp90 with EC50 of 62±29 nM.
BAY 11-7082 is a NF-κB inhibitor which decreases NF-κB by inhibiting TNF-α-induced phosphorylation of IκB-α. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50s of 0.19 μM and 0.96 μM, respectively.
Pemetrexed disodium heptahydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
5'-O-DMT-N2-isobutyryl-2'-O-propargylguanosine 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].
NVP-2 is a CDK9 inhibitor with an IC50 of 0.5 nM.
(+)-CBI-CDPI2 is an enhanced functional analog of CC-1065. (+)-CBI-CDPI1 is a DNA alkylating agent. (+)-CBI-CDPI2 is an antibody drug conjugates (ADCs) toxin.
8-(Methylamino)adenosine 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].
GW 6471 is a potent PPARα antagonist.
2’-Deoxy-2’-fluoro-N3-(4-nitrobenzyl)-beta-D-arabinouridine 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].
PARP10-IN-3 is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10. PARP10-IN-3 reveals potent inhibition on PARP2 and PARP15 with IC50s of 1.7 μM for human PARP2 and human PARP15, respectively[1].
Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes[1]. Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties[2].
H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner[1][2].
eIF4A3-IN-15 (compound 52) is a silvestrol (HY-13251) analogue. eIF4A3-IN-15 interferes the assembling of eIF4F translation complex with EC50s of 11, 700 and 120 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-15 can be used for the research of human cancer pathogenesis[1].
Mitomycin C is an antitumor drug and antibiotic that shows extraordinary ability to inhibit DNA synthesis.
GRP78-IN-2 (Compound FL5) is a GRP78 (Glucose Regulated Protein 78 kDa) inhibitor. GRP78-IN-2 preferentially targeting cell surface GRP78 and shows potent antiangiogenic and anticancer activities without affecting other normal cells[1].
Thymidine-13C 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]
PSTAIR is a monoclonal antibody that recognizes the PSTAIR sequence in Cdc28, PSTAIR can be used as loading control[1].
Apratoxin A, a cyanobacterial metabolite, mediates antiproliferative activity through the induction of G1 cell cycle arrest and an apoptotic cascade. Apratoxin A associates with Hsp70/Hsc70 to promote the degradation of Hsp90 client proteins. Apratoxin A can specifically bind the Sec61 complex[1][2][3].