CCT020312 is capable of delivering potent, and eukaryotic initiation factor 2-alpha kinase 3 (EIF2AK3) selective, proliferation control and also is an activator of RNA-like endoplasmic reticulum kinase (PERK).
3-Deoxy-1,2:5,6-bis-O-(1-methylethylidene)-α-D-ribo-hexofuranose 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].
3’-O-(2-Methoxyethyl)-2-thiouridine 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].
GW9578 is a subtype-selective PPARα agonist (EC50s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity[1][2].
UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM[1].
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research[1].
2’,3’-Bis-(O-t-butyldimethylsilyl)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].
Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death[1].
5'-ODMT cEt m5U Phosphoramidite Amidite is a locked nucleic acid (LNA) analog. 5'-ODMT cEt m5U Phosphoramidite Amidite shows excellent safety and antisense activity[1][2].
2-Aminopurine-9-beta-D-(3’,5’-di-O-benzoyl-2’-deoxy-2’-fluoro)arabinoriboside 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].
L-Threonolactone ((3R,4S)-3,4-Dihydroxyoxolan-2-one) 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-26 is a highly selective class I HDAC inhibitor with an EC50 value of 4.7 nM.
6-Mercaptopurine-13C2,15N (Mercaptopurine-13C2,15N) is the 13C- and 15N-labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate is a PPARα agonist[1].
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice[1].
Doxifluridine-d2 is the deuterium labeled Doxifluridine[1]. Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
BAY 1161909 is a potent Mps1 inhibitor, with an IC50 of < 1 nM.
2’-Deoxy-N6-(3-methoxybenzyl)adenosine 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].
T-peptide is a peptide derived from microtubule binding repeat of Tau protein. T-peptide self-assembles into 30-55 nm paired helical filaments (PHFs) even in the absense of inducers. T-peptide is cytotoxic in multiple cell lines including cortical neurons, cerebellar granular neurons, neuroblastoma cells, kidney fibroblasts and HEK293 cells. T-peptide co-localizes with pathological hyperphosphorylated forms of tau in vitro.
PU-H71 is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
N,N-Dimethyl-2’-O-methylcytidine 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-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.
Wistin, isolated from Caragana sinica roots, is a PPARα and PPARγ agonist[1][2].
Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, 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].
USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of less than about 50 nM[1].
Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1].
Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii[1].
1-Hydroxyanthraquinone, a naturally occurring compound with oral activity from some plants like Tabebuia avellanedae, exhibits carcinogenic effect[1].
2′-Deoxy-2-iodoadenosine 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-Chloro-2'-deoxycytidine 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].