CDK2-IN-11 (compound 9d) is a potent CDK2 inhibitor with an IC50 of 6.4 μM, and KI values of 23.4 nM, 56.3 nM and 44.3 nM for hCA II, hCA IX and hCA XII, respectively. CDK2-IN-11 can be used for researching anticancer[1].
Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity[1].
2',3'-Dideoxyuridine 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].
Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork[1][2].
Phomopsin A is a cyclic hexapeptide mycotoxin isolated from the fungus Phomopsis leptostomiformis. Phomopsin A is a noncompetitive inhibitor of the binding of radiolabeled vincristine to tubulin[1].
Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies[1][2][3].
Erythromycin lactobionate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin lactobionate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin lactobionate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride restricts uterine DNA synthesis and function in mice[1][2][3][4].
Tubastatin A (TSA) TFA is a potent and selective?HDAC6?inhibitor with?IC50?of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A TFA also inhibits HDAC10 and metallo-β-lactamase domain-containing protein?2 (MBLAC2).
1-(2-C-β-Methyl-β-D-ribofuranosyl)-5-nitropyridine-2(1H)-one is a nitropyridine nucleoside analogue.
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase ((DYRK)) inhibitor with anticancer and anti-inflammatory activities.
Haspin-IN-3 (compound 8l) is a potent haspin inhibitor with IC50 of 14 nM. Haspin-IN-3 has anticancer effects[1].
2’,3’,5’-Tri-O-acetyl-5-methoxycarbonylmethyl-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].
N-Acetyl-2′-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].
LY2880070 is an orally active CHK1 inhibitor. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents[1].
Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.
5-Formylindole-CE phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Tubercidin (7-Deazaadenosine) is an adenosine analog, is an antibiotic obtained from Streptomyces tubercidicus.Target: AntibacterialTubercidin inhibits the growth of Streptococcus faecalis by 50 % at a concentration of 20 nM. Tubercidin is not subject to cleavage by adenosine phosphorylase or to deamination by adenosine deaminase. The antibiotic served as a substrate for numerous enzymes involved in the anabolism of adenosine, as demonstrated by its incorporation into RNA and DNA, and by the formation of nicotinamide-deaza-adenine dinucleotide. Tubercidin proves to be a weak inhibitor of adenosine phosphorylase, and interfered with the phosphorylation of adenosine and AMP. The inhibition of the growth of S. faecalis by Tubercidin is prevented by purine and pyrimidine nucleosides, ribose 5-phosphate, pyruvate, and certain amino acids. In the presence of Tubercidin, growing cultures of the test organism used pyruvate instead of glucose, whereas in the absence of the antibiotic glucose served as the main source of energy. It is suggested, therefore, that the impairment of growth is due primarily to the interference of Tubercidin with the utilization of glucose.
MC-DOXHZN hydrochloride is an albumin-binding prodrug of Doxorubicin, with acid-sensitive properties[1].
5-Propargylamino-ddUTP, a nucleoside molecule that can be used to synthesis of cyanine dye-nucleotide conjugate which is used in nucleic acid labeling or sequence analysis[1].
2’-O-Acetyl-3’,5’-bis-O-benzoyl-6-aza-xylo 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].
G244-LM is a potent and specific inhibitor of tankyrase 1/2 that inhibits Wnt signaling[1].
Pemetrexed 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.
Tubulin inhibitor 20 (compound 1) is a potent inhibitor of tubulin. Tubulin inhibitor 20 has the potential for the research of cancer diseases[1].
YKL-1-116 is a potent, selective and covalent inhibitor of CDK7 that does not inhibit other CDKs; synergizes with 5-FU or nutlin-3 to kill HCT116 cells, produces dose-dependent increases in PARP cleavage; is more potent than THZ1 towards both Cdk7WT and Cdk7as (analog-sensitive mutant).
CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research[1].
Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic[1].
3’-beta-C-Methyluridine 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].
Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, 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].
LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC50=55 nM) with180-fold selectivity verses DYRK2 (IC50=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455)[2].