T6157

Devimistat (6,8-Bis(benzylthio)octanoic acid) , a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. It has potential chemopreventive and antineoplastic activities, and has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Advanced Cancer, and Pancreatic Cancer, among others.

USP15-IN-1 is a potent USP15 inhibitor (IC50 is 3.76 μM) with high antiproliferative activity against non-small cell lung cancer and leukemia cells. As an interacting protein of cGAS, USP15 promotes cGAS to recognize DNA and activate downstream signaling pathways.

Mt KARI-IN-2 (compound 5b) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki value of 2.02 μM. It also inhibits Mtb H37Rv with a MIC value of 0.78 μM and demonstrates low cytotoxicity, as indicated by a HEK IC50 greater than 86 μg/mL [1].

FNDR-20123 free base, a pioneering and orally administered anti-malarial agent, acts as a Histone Deacetylase (HDAC) inhibitor, displaying potent efficacy with IC50 values of 31 nM for Plasmodium and 3 nM for human HDAC, respectively. It effectively targets both the asexual (IC50=41 nM) and sexual blood stages (IC50=190 nM for male gametocytes) of Plasmodium falciparum. Additionally, FNDR-20123 free base inhibits multiple HDAC isoforms, namely HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with respective IC50 values of 25, 29, 2, 11, and 282 nM, and displays nanomolar inhibitory concentrations against Class III HDAC isoforms [1].

MtTMPK-IN-5 (compound 17) is a highly effective inhibitor of M. tuberculosis thymidylate kinase (Mtb TMPK), demonstrating remarkable enzyme inhibitory activity with an IC50 of 34 μM. Additionally, MtTMPK-IN-5 exhibits notable activity against M. tuberculosis, with an MIC of 12.5 μM. Given its potent properties, MtTMPK-IN-5 serves as a valuable tool for tuberculosis research [1].

Anticancer Agent 83, a potent inhibitor of LOX IMVI cell growth, demonstrates anticancer efficacy with a GI50 value of 0.15 mM. It disrupts mitochondrial membrane potential and induces DNA damage, thereby promoting apoptosis in leukemia cells [1].

Sulfinalol is a compound that acts as an orally active β-adrenoceptor antagonist and directly induces vasodilation [1].

BRD3731 is a selective inhibitor of GSK3β, demonstrating an IC50 value of 15 nM for GSK3β and 215 nM for GSK3α. Due to its inhibitory properties, BRD3731 holds promise for investigating various medical conditions, including post-traumatic stress disorder (PTSD), psychiatric disorders, diabetes, and neurodegenerative disorders [1].

BuChE-IN-5 (compound 25b) is a highly potent BuChE inhibitor with an IC50 value of 1.94 μM, effectively inhibiting Aβ and tau protein aggregation in Escherichia coli, and demonstrating significant free radical scavenging and antioxidant activity, making it a valuable tool for Alzheimer's disease research [1].

Devimistat-D10 is the deuterium-labeled form of Devimistat (T6157).