Dihydro-5-azacytidine (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine has an antitumor activity[1][2].
EB-47, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD+ and extends from the nicotinamide to the adenosine subsite[1].
LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis[1][2][3].
Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response[1][2].
3’-Deoxy-5-methoxyuridine 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].
SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect[1].
N4-Benzo yl-5’-O-(4,4’-dimethoxytrityl)-aracytidine 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-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer[1].
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect[1].
2’-O-Me-2-thio-U-3’-phos phoramidite 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].
Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
HBV-IN-21 (Compound II-8b) is an HBV DNA replication inhibitor with an IC50 of 2.2 µM. HBV-IN-21 can interact HBV 4 capsid protein with good affinity (KD = 60.0 μM)[1].
Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells[1][2][3].
8-Benzyloxyadenosine 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].
T-2 Toxin (T-2 Mycotoxin) is a toxic trichothecene mycotoxin produced by various Fusarium species in feedstuffs and cereal grains, LD50 values of T-2 Toxin in mice and rats are 5.2 and 1.5 mg/kg BWa,respectively [1]. T-2 Toxin (T-2 Mycotoxin) can be transformed into a variety of metabolite, the typical metabolites of T-2 toxin in animals are HT-2 toxin and T-2-triol, which are hydrolysates[1]. T-2 Toxin (T-2 Mycotoxin) is an inhibitor of protein synthesis resulting from binding peptidyltransferase, which is an integral part of the 60s ribosomal subunit. T-2 Toxin (T-2 Mycotoxin) inhibits the synthesis of DNA and RNA, interferes with the metabolism of membrane phospholipids, and increases the level of liver lipid peroxides[1]. T-2 Toxin (T-2 Mycotoxin) induces apoptosis in the immune system, gastrointestinal tissues, and fetal tissues[2].
KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell[1].
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
M3814 is a potent and selective inhibitor of DNA-dependent Protein Kinase (DNA-PK).
Synstab A is a mitosis modulator to promote interactions between α- and β-tubulin. Synstab A can polymerizes microtubules from purified tubulin, and produces microtubule bundles in interphase cells[1][2].
ODN BW001 is an oligodeoxynucleotide (ODN). ODN BW001 plays a regulatory role in the proliferation and activation of osteoblast[1][2].
Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].
2-Aminoadenosine 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].
2′,5′-Dideoxy-5′-iodouridine 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].
CDK2-IN-15 (Compound 19) is an inhibitor of CDK2 with an IC50 of 2.9 μM. CDK2-IN-15 can be used for cancer research[1].
M4076 is a higly potent, selective, ATP-competitive inhibitor of ATM kinase with IC50 of 0.2 nM.M4076 sensitizes tumor cell lines to radiation therapy in vitro and strongly enhances the anti-tumor activity of ionizing radiation in vivo.
Niraparib (MK-4827) is a highly potent PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively.
N-Acetyladenosine 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].
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats[1].
5-Vinylcytidine 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].