EC1454 is an anti-tumor compound, extracted from US20170348376A1[1].
5-Methoxyuridine 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].
Sucralose is an intense organochlorine artificial sweetener.
GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
FLX475 is a potent CCR4 antagonist that blocks regulatory T cells that interfere with effective antitumor immune responses and has antitumor activity[1].
Trebananib (2xCon4C; AMG 386), a non-VEGF-dependent angiogenesis pathway inhibitor, is a peptide-Fc fusion protein that neutralises the interaction between angiopoietins-1/2 and the Tie2 receptor, plus FOLFIRI. Trebananib can be used to research anticancer and ocular neovascular diseases[1][2].
[10]-Shogaol is an antioxidant from Zingiber officinale for human skin cell growth and a migration enhancer. [10]-Shogaol inhibits COX-2 with an IC50 of 7.5 μM and has antiproliferation activity[1][2][3].
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer[1].
Deoxythymidine-5'-triphosphate (dTTP), a deoxynucleotide, can be used in deoxyribonucleic acid synthesis[1].
NSC 228155 is a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM. NSC 228155 is not selective against CREB-mediated gene transcription in living HEK 293T cells[1].
NNK-d3 is the deuterium labeled NNK (HY-126477)[1][2].
CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity[1].
PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase[1].
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential[1][2].
ICMT-IN-9 (compound 47) is an inhibitor of ICMT (IC50=0.16 μM)[1].
hCAII-IN-3 (compound 7e) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 124.2 and 30.5 nM, respectively. hCAII-IN-3 has the potential for the research of cancer diseases[1].
Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor for treating disorders associated altered cell migration, such as cancer.
HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC50 value of 6nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders[1].
Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination[1].
Grisnilimab setaritox (WT1-RTA), is an antihuman T cell antibody (anti-CD7) conjugating with ricin A chain (RTA). RTA is a 30-kDa peptide capable of rapidly in activating ribosomal 60S subunits. Grisnilimab setaritox is cytotoxic to CEM (T-lymphoblastic leukemia) cells in vitro with an ID50 of 53 pM. Grisnilimab setaritox also improves leukemic meningitis model in rhesus monkeys[1].
Methylmalonic acid-13C4 is the 13C labeled Methylmalonic acid[1]. Methylmalonic acid (Methylmalonate) is an indicator of Vitamin B-12 deficiency in cancer[2].
Tezatabep matraxetan is a radiolabeled polypeptide used for diagnosis and research of cancer characterized by overexpression of HER2[1].
Yakuchinone A is a natural product isolated from the fruit of Alpinia oxyphylla, which can induce apoptosis and has anticancer and anti-inflammatory activities[1].
5'-Protected 2,2'-anhydrouridine 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].
Bim 21009 is an inhibitor of gonadorelin.
HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models[1].
BI 853520 (IN-10018) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). BI 853520 shows anti-proliferative activity against cancer cells[1][2].
AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis[1].