5’-O-DMTr-3’-deoxyuridine 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].
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects[1][2][3].
2’-O-Hexadecanyl guanosine 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].
Tubulin polymerization-IN-57 (compound 5a) is a tubulin inhibitor and is an α-naphthoxy-substituted carbendazim (HY-13582) derivative. Tubulin polymerization-IN-57 induces mitotic arrest and inhibits cancer cell proliferation[1].
DMT-2'O-Methyl-rC(tac) Phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
2,3’-Anhydrothymidine; 2’-Deoxy-3’,2-anhydro-5-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].
Demethoxyfumitremorgin C is a secondary metabolite of the marine fungus, Aspergillus fumigatus. Demethoxyfumitremorgin C induces prostate cancer cell apoptosis. Demethoxyfumitremorgin C activates caspase-3, -8, and -9, leading to PARP/ cleavage[1].
N6-Methyl-2’-β-C-methyladenosine 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].
Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
Bendamustine hydrochloride is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
trans-Coniferyl aldehyde (compound 2) is a natural compound isolated from the buds of clove (Syzygium aromaticum).trans-Coniferyl aldehyde suppresses 63% of the UV mutable gene expression at 1.20 μM, and with an ID50 value of 0.76 μM,and has the antimutagenicactivities against furylfuramide, Trp-P-1, and activated Trp-P-1[1].
3’-Deoxy-3’-fluoro-xyloguanosine 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].
4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide is used to treat lymphomas and autoimmune disorders.
8-Azido-ADP (disodium) is a covalent-binding inhibitor of mitochondrial adenine nucleotide translocation. 8-Azido-ADP (disodium) causes irreversible inhibition of adenine nucleotide exchange in a light-dependent reaction. 8-Azido-ADP (disodium) inhibits the normal state 4 → 3 transitions of mitochondrial respiration induced by ADP[1].
CDDD2-94 is a highly potent and selective CDK4 inhibitor with Ki of 2 nM, >140-fold selective for CDK4 over CDK6 (Ki=279 nM).CDDD2-94 is ineffective against other members of the CDK family, displays high selectivity against a panel of 369 human kinases at 1uM, with exceptionally selective-CLK, DYRKs and MYLK4 were the only kinases targeted potently.CDDD2-94 is the most selective CDK4 inhibitor identified to date.CDDD2-94 demonstrated antiproliferative activityagainst MV4-11 and MDA-MB-453 cell lines with GI50 of 0.107 and 0.325 uM respectively.CDDD2-94 inhibits S780-phosphorylated Rb (pRb(S780)) and decreases transcription of Rb1 and E2F-target genes in MDA-MB-453 cells.CDDD2-94 is well tolerated and efficacious in preclinical OC xenograft model, CDDD2-94 provides better safety profile than palbociclib towards the bone marrow.
Kif15-IN-2 is an inhibitor of the mitotic kinesin Kif15, and is used for the research of cellular proliferative diseases.
3-Deazauridine (NSC 126849) is a uridine analogue. 3-Deazauridine competitively inhibits cytidine triphosphate synthase to inhibit the biosynthesis of cytidine-5'-triphosphate. 3-Deazauridine acts synergistically with several antineoplastic agents, acting as a biological response modifier[1].
HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitory activity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitory activity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer[1].
Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells[1][2].
Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential anti-tumour activity[1].
KIF18A-IN-1 is a mitotic kinesin KIF18A inhibitor extracted from patent WO2021026098A1 example 100-13. KIF18A-IN-1 exhibits anti-tumor activity[1].
5-Ethyl cytidine is a cytidine 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].
2′-Amino-2′-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].
5-Fluoro-1-((2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione (2',5-difluoro-2'-deoxy-1-arabinosyluracil) is a uridine analogue. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC)[1].
5-Fluoro-4’-C-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].
2’-O-Hexadecanyl-2-aminoadenosine 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].
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model[1].
5’-O-DMTr-2’,2’-difluoro-dC(Bz)-3’-CED-phosphoramidite 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].
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM[1][2].