carcinomas

Nutlin-3a is the active enantiomer of Nutlin-3, an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3a binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3a has antitumor activity.

K-Ras-IN-1, a K-Ras inhibitor, is characterized by its chemical formula C20H19ClN4O2S and is also known as N-[(1S)-3-cyclopropyl-1-[(6-fluoro-1H-benzimidazol-2-yl)sulfanyl]-2-oxo-1-(phenylmethyl)propyl]-4-fluorobenzenesulfonamide (compound [18, dashboard 819041] in brackets).

Germinone A (3-Methyl-5-((3-nitro-[1,1'-biphenyl]-4-yl)oxy)furan-2(5H)-one) is a novel potent agonist of HTL KAI2, stimulating activity for Arabidopsis seed germination, has antitumor activity in multiple types of carcinomas.

HPV16 E7 (86-93) acetate is a derived peptide of human leukocyte antigen A2.1 restricted HPV16 E7 with immunogenic property in cervical carcinomas.

N-Nitroso-N-methyl-4-aminobutyric acid (NMBA) is a tobacco-specific nitrosamine carcinogen.1It is oxidized to the reactive metabolite methyl-2-oxopropylnitrosamine (MOPN) in isolated rat liver mitochondria.2NMBA induces bladder transitional cell carcinomas in rats when administered in the drinking water at a concentration of 300 mg/L per day.3

Garcinone E is active constituents in the anticomplement assay used. Garcinone E exhibits potent activity in vitro against Plasmodium falciparum chloroquine-resistant strain W2, with IC50 values below 3 µM. It has potent cytotoxic effect on all hepatocellular carcinomas cell lines as well as on the other gastric and lung cancer cell lines included in the screen, may be potentially useful for the treatment of certain types of cancer.

N-Nitroso sarcosine is a carcinogen and nitrosation product of sarcosine that has been found in cured meat products.1,2In vivo, N-nitroso sarcosine (225 mg/kg) induces the formation of metastatic liver carcinomas in mice.2 1.Janzowski, C., Eisenbrand, G., and Preussmann, R.Occurrence of N-nitrosamino acids in cured meat products and their efffect on formation of N-nitrosamines during heatingFood Cosmet. Toxicol.16(4)343-348(1978) 2.Wogan, G.N., Paglialunga, S., Archer, M.C., et al.Carcinogenicity of nitrosation products of ephedrine, sarcosine, folic acid, and creatinineCancer Res.35(8)1981-1984(1975)

FMOC-L-THR (AZP-531) is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight. The O-glycosidic linkage and the O-acetyl protection in this building block is stable to both piperidine and TFA, making it completely compatible with standard protocols in Fmoc solid phase peptide synthesis. The Tn antigen is a tumor-associated carbohydrate antigen that is not normally expressed in peripheral tissues or blood cells. Expression of this antigen, which is found in a majority of human carcinomas of all types, arises from a blockage in the normal O-glycosylation pathway in which glycans are extended from the common precursor GalNAcα1-O-Ser Thr (Tn +antigen)[1].

Ganglioside GT1b is a trisialoganglioside that is characterized by having two sialic residues linked to the inner galactose unit. It binds to the neurotoxins botulinum toxin serotype A (BTxA), BTxA heavy chain, and tetanus toxin with IC50 values of 11, 0.74, and 7.2 μM, respectively.[1] Ganglioside GT1b-containing liposomes bind to the major coat protein VP1 from Merkel cell polyomavirus (MCPyV), which has been identified in Merkel cell carcinomas, identifying ganglioside GT1b as a putative MCPyV receptor. [2] Ganglioside GT1b decreases production of IL-6, IL-10, IgG, IgM, and IgA in human peripheral blood mononuclear cells (PBMCs) by 31.4, 30.5, 60, 59.5, and 58%, respectively, when used at a concentration of 10 μM [3] . Ganglioside GT1b mixture contains ganglioside GT1b molecular species with C18:1 and C20:1 sphingoid backbones.

Potent endogenous ligand of the kisspeptin receptor (KISS1, GPR54). Binds with high affinity to rat and human KISS1 receptors with Ki values of 1.80 and 1.45 nM respectively. Inhibits chemotaxis, invasion and metastasis of human melanomas and breast carci

Diuron is a Phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (25 nM/ml) decreases total respiration in roots of wheat by 50% and ground respiration by 100%. Diuron (2,500 ppm, dietary) increases the inc

AMPK Activator 11 is a nanomolar potent inhibitor of cell proliferation in various colorectal carcinomas (CRCs), acting through the selective activation of AMP-activated protein kinase (AMPK) and enhancement of oxidative phosphorylation (OXPHOS) (mitochondrial metabolism). This compound demonstrates particular efficacy in inhibiting RKO xenograft growth, rendering it useful for anti-tumor and metabolic disease research [1].

Lewis Y Tetrasaccharide (Lewis Y, Le Y) is a tetrasaccharide derivative of Lewis X Trisaccharide, functioning as an antigen linked to the metastasis of malignant ovarian carcinomas and associated with a poor prognosis [1] [2].

ReACp53 is a cell-penetrating peptide, designed to inhibit p53 amyloid formation, resues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC).

Arotinoid (RO 13-6298), a highly potent retinoid, functions as an orally active agonist of retinoic acid receptors (RARs) and exhibits antipsoriatic properties. It demonstrates antipapilloma activity, having an ED 50 of 0.05 mg kg. Arotinoid is also employed in the research of skin carcinomas [1] [2].

Mitopodozide, as an ethylhydrazide derivative of podophyllic acid, acts as a mitotic poison in carcinomas of the ovary.

KRAS G12D Inhibitor 16 is a potent compound targeting the KRAS G12D and its mutation, exhibiting inhibitory activity with IC50 values of 0.7 nM and 0.35 μM, respectively. It is utilized in researching various malignant tumors including pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), and non-small cell lung carcinomas (NSCLC).

Heptadecanoic acid is a fatty acid of exogenous (primarily ruminant) origin. Many odd length long chain amino acids are derived from the consumption of dairy fats (milk and meat). Heptadecanoic acid constitutes 0.61% of milk fat and 0.83% of ruminant me

HPV16 E7 (86-93) TFA, a peptide derived from HPV16 E7, is restricted by human leukocyte antigen (HLA)-A2.1 and exhibits immunogenic properties in cervical carcinomas [1] [2].

Dalpiciclib (SHR-6390) hydrochloride is a highly selective, orally active CDK4 6 inhibitor with IC50 values of 12.4 nM and 9.9 nM, respectively, acting as an antitumor agent in breast and esophageal squamous cell carcinomas.

Polyphyllin G (Polyphyllin VII), the the main member of polyphyllin family, shows strong anticancer activity against several carcinomas, including lung cancer, breast cancer, colorectal cancer, cervical cancer, hepatocellular carcinoma and osteosarcoma.

TYRA-300 is an oral and selective FGFR3 inhibitor with an IC50 value of 11 nM and 25-fold, 14-fold, and 36-fold selectivity for FGFR1, FGFR2, and FGFR4, respectively, in the Ba F3 cell line for the treatment of metastatic uroepithelial carcinomas (mUCs) and chondrodysplasia.