3’-beta-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].
5-Methyl-2-thiouridine (2-Thio-5-methyluridine) 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].
Riviciclib hydrochloride (P276-00) is a potent CDK9-cyclinT1, CDK4-cyclin D1, CDK1-cyclinB, CDK2-cyclin A, CDK2-cyclin E, CDK6-cyclin D3, and CDK9-cyclin H inhibitor with IC50 values of 20 nM, 63 nM, 79 nM, 224 nM, 2500 nM, 396 nM, 2900 nM, respectively[1].Riviciclib hydrochloride shows antitumor activity on cisplatin-resistant cells[3].
RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM.IC50 Value: 5-30 μMTarget: RAD51in vitro: RI-1 sensitizes cells to DNA damage by directly and specifically disrupting HsRAD51 and inhibiting the ability of RAD51 to form filaments on ssDNA. In addition, RI-1 alone generates single-agent toxicity in all three cancer cell lines (HeLa, MCF-7 and U2OS) with LD50 values in the 20–40 μM range. RI-1 decreases the rejoining of γ-H2AX foci in G2 phase cells and results in a higher level of unrepaired DSBs 6 hours after irradiation. in vivo:
Bimolane (AT-1727), a human topoisomerase II inhibitor, can be used as an anti-neoplastic agent and for the research of psoriasis. Bimolane shows leukemogenic activity and induces multiple types of chromosomal aberrations in human lymphocytes[1][2].
KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively[1].
4’-C-Methyl-5-methoxyuridine 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].
5-Aza-3’-deoxycytidine 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].
Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin[1][2][3].
Akt1&PKA-IN-2 ((R)-29) is an inhibitor of PKB/AKT with cyclin-dependent kinase 2 (CDK2) selectivity. Akt1&PKA-IN-2 inhibits AKT1, PKAa and CDK2a with IC50 values of 0.007 µM, 0.01 µM and 0.69 µM, respectively[1].
4-Methoxy-1-β-D-ribofuranosyl-1H-pyrazolo[3,4-d]pyrimidin-6-amine 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].
N1-Allylpseudouridine 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].
Retaspimycin Hydrochloride is a potent and water-soluble inhibitor of Hsp90 with EC50s of 119 nM for both Hsp90 and Grp9.
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].
Tubulin polymerization-IN-41 is a potent tubulin polymerization inhibitor with the IC50 of 2.61 μM. Tubulin polymerization-IN-41 targets the Colchicine-binding site of tubulin. Tubulin polymerization-IN-41 has anticancer effects[1].
Tubulysin G is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin G is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
Sirtuin modulator 2 (Compound 132) is a sirtuin modulator with an ED50 equal or less than 50 μM[1].
CDK4/6-IN-7 is a potent, selective and orally active CDK4/6 inhibitor, with IC50s of 1.58 and 4.09 nM, respectively. CDK4/6-IN-7 can be used for the research of breast cancer[1].
NHC-triphosphate is an intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate is a weak alternative substrate for the viral polymerase and changes the mobility of the product in polyacrylamide electrophoresis gels[1].
5'-Deoxy-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].
5-Fluoro-2′-deoxy-UTP can be used as a substrate for DNA synthesis[1].
AZD1390 is an ATM inhibitor.
Ascamycin is a 5'-O-sulfonamide ribonucleoside antibiotic produced by Streptomyces sp. JCM9888. Ascamycin has a selective antibacterial activity against Xanthomonas species with MIC values of 0.4 μg/mL, 12.5 μg/mL and 12.5 μg/mL for Xanthomonas citri, Xanthomonas oryzae and Mycobacterium phlei, respectively[1][2][3].
B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
m7GpppAmpG is a trinucleotide cap analog with the capping efficiencies for the obtained RNAs of 90%[1].
HDAC-IN-29 (compound 13b) is a potent pan-HDAC inhibitor. HDAC-IN-29 shows antitumor activity[1].
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].
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].
ATR-IN-13 (compound A9) is a potent ATR kinase inhibitor, with an IC50 of 2 nM. ATR-IN-13 can be used for ATR kinase mediated diseases research, such as proliferative diseases and cancer[1].
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].