MTDIA (also known as MT-DADMe-ImmA and Methylthio-DADMe-Immucillin A) is a novel and potent inhibitor of human 5′-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. Human 5′-methylthioadenosine phosphorylase (MTAP) is solely responsible for 5′-methylthioadenosine (MTA) metabolism to permit S-adenosylmethionine salvage. Transition-state (TS) analogues of MTAP are in development as anticancer candidates. TS analogues of MTAP […]

Arfolitixorin, an intravenously administered folate-based compound, is a novel and potent antifolate modulator that is being developed by Isofol Medical AB, for the treatment of cancer. Arfolitixorin, [6R]-5,10-methylene-tetrahydrofolic acid, is being developed to increase the efficacy of 5-FU, which has been shown to be a cytotoxic agent, as well as a rescue drug after methotrexate […]

Methyl protodioscin (also known as NSC-698790; Smilax saponin B) is a novel furostanol bisglycoside with potent antitumor properties; it is able to reduce proliferation and cause cell cycle arrest.

PI3Kα/mTOR-IN-1, a 4-methylpyrido pyrimidinone (MPP) analog, is a novel and potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

BI-3663 is a novel, potent, functional and highly selective PTK2/FAK degrader based on PROTAC (proteolysis-targeting chimeras) technology, utilizing VHL (von Hippel-Lindau) and cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. Focal adhesion tyrosine kinase (PTK2) is often overexpressed in human hepatocellular carcinoma (HCC), and several […]

WAY-100135 (WAY100135) is a novel and potent serotonergic drug of the phenylpiperazine family for scientific research. It acts as potent 5-HT1A receptor antagonist, and was originally believed to be highly selective, but further studies have demonstrated that it also acts as a partial agonist of the 5-HT1D receptor (pKi = 7.58; virtually the same affinity […]

SB 258719 (SB-258719) is a novel, potent and selective 5-HT7 receptor antagonist with a pKi of 7.5. Both SB-258719 and mesulergine displayed apparent partial inverse agonist profiles compared to the other antagonists tested. These inhibitory effects of antagonists appear to be 5-HT7 receptor-mediated and to reflect inverse agonism.

SJG-136 (NSC694501), a novel sequence-selective pyrrolobenzodiazepine (PBD) dimer, is a novel and potent DNA cross-linking/intercalating agent with an XL50 of 45 nM for pBR322 DNA; SJG-136 has potent anticancer activity and can be potentially used for the treatment of ovarian cancer and leukemia.

NSC305787 HCl, the hydrochloride salt of NSC305787, is a novel, potent and selective small molecule inhibitor of ezrin with a Kd of 5.85 μM, it inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, and has antitumor activity. Ezrin is a key driver of tumor progression and metastatic spread of […]

JNJ-47117096 HCl (also known as MELK-T1), identified from a fragment-based drug design, is a novel, potent and selective MELK (maternal embryonic leucine zipper kinase) inhibitor with an IC50 of 23 nM, it also effectively inhibits Flt3, with an IC50 of 18 nM. Maternal embryonic leucine zipper kinase (MELK), a serine/threonine protein kinase, has oncogenic properties […]