(-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro[1].
Hydrolyzed Fumonisin B1 (Aminopentol) is the backbone and main hydrolysis product of the mycotoxin fumonisin B1 (FB1), can weakly inhibit ceramide synthase[1].
MMP-9-IN-4 is a MMP-9 inhibitor (IC50: 7.46 nM) that has H-π interactions with MMP-9. MMP-9-IN-4 also inhibits AKT activity (IC50: 8.82 nM). MMP-9-IN-4 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-4 can be used in the research of cancers[1].
Mimosine, a tyrosine analog , can act as an antioxidant by its potent iron-binding activity[1]. Mimosine is a known chelator of Fe(III)[2]. Mimosine induces apoptosis through metal ion chelation, mitochondrial activation and ROS production in human leukemic cells[3]. Anti-cancer, antiinflammation.
Mitotane-d8 is the deuterium labeled Mitotane[1]. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has drug-drug interactions[2][3][4][5].
Pomstafib-2 is a potent and selective STAT5b inhibitor. Pomstafib-2 decreases the expression of pSTAT5b and induces Apoptosis[1][2].
Kurzipene D (compound 4) is a potent anticancer agent. Kurzipene D induces the apoptosis and arrested the HepG2 cell cycle at S stage. Kurzipene D shows anti-tumor effects using in vivo zebrafish model. Kurzipene D has the property of inhibiting tumor proliferation and migration[1].
Tubulin polymerization-IN-56 (compound 8l), an indazole derivative, is a potent tubulin polymerization inhibitor through interacting with the colchicine site, resulting in cell cycle arrest and cellular apoptosis. polymerization-IN-56 reduces cell migration and leads to more potent inhibition of tumor growth in vivo[1].
(E/Z)-Squalene ((E/Z)-Super Squalene; (E/Z)-AddaVax) is a triterpenic compound. (E/Z)-Squalene accumulates and reduces liver cholesterol and triglycerides in the liver. (E/Z)-Squalen regulates the production of intracellular active oxidants (ROS) and induces apoptosis and necrosis in a concentration-and time-dependent manner[1].
(S)-Crizotinib, a (S)-enantiomer of crizotinib, is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models[1].
Oxcarbazepine-d4-1 is deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker[1]. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines[2]. Anti-cancer and anticonvulsant effects[2][3].
Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines，and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines)[1].
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase[1].
7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities[1][2].
Melittin free acid is a basic 26-amino-acid polypeptide, the major active ingredient of honeybee venom. Melittin free acid is an activator of phospholipase A2 (PLA2). Melittin free acid has broad-spectrum antifungal activity with MIC values of 0.4-60 μM. Melittin free acid hinders fungal growth by inducing cell apoptosis, repressing (1,3)-β-D-glucan synthase and participating in other pathways[1][2].
3-Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-Dehydrotrametenolic acid induces apoptosis and has anticancer activity[1][2].
Orlistat is a lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats.
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression[1].
Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
α-Tocopherol phosphate (alpha-Tocopherol phosphate) disodium, a promising antioxidant, can protect against long-wave UVA1 induced cell death and scavenge UVA1 induced ROS in a skin cell model. α-Tocopherol phosphate disodium possesses therapeutic potential in the inhibition of apoptosis and increases the migratory capacity of endothelial progenitor cells under high-glucose/hypoxic conditions and promotes angiogenesis[1][2].
2,4,6-Triiodophenol is an orally active and potent leukotriene B4 (LTB4) synthesis inhibitor. 2,4,6-Triiodophenol can induce mouse blastocysts apoptosis[1][2].
Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina[1][2][5].
GK563 is a selective Ca2+-independent phospholipase A2 (GVIA iPLA2) inhibitor with an IC50 value of 1 nM. GK563 is 22000 times more active against GVIA iPLA2 than GIVA cPLA2. GK563 reduces β-cell apoptosis induced by proinflammatory cytokines, raising the possibility that it can be beneficial in countering autoimmune diseases, such as type 1 diabetes[1].
Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models[1].
5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis[1][2].
STAT3-IN-10 (A11) is a STAT3 inhibitor with an IC50 value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, inhibits tumor cell growth and induces apoptosis in cancer cells[1].
RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with 50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[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].
Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL[1][2][3][4][5].
Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation[1].