CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity[1].
(S)-(−)-Perillyl alcohol is a monoterpene found in lavender, inhibits farnesylation of Ras, upregulates the mannose-6-phosphate receptor and induces apoptosis. Anti-cancer activity[1].
Batabulin sodium (T138067 sodium) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin sodium affects cell morphology and leads to cell-cycle arrest ultimately induce apoptotic cell death. Batabulin sodium has efficacy against multidrug-resistant (MDR) tumors[1].
2-HBA is a potent inducer of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1) which can also activate caspase-3 and caspase-10.
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis[1][2].
Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity[1][2][3].
SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 µM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity[1].
DCG066 is a G9a inhibitor in vitro.
Ammonium iron(III) citrate (Ammonium ferric citrate), a physiological form of nonetransferrin-bound iron, induces intracellular iron overload to cause ferroptosis[1]. Ammonium iron(III) citrate can enhance protein production[2].
Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with drug-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9[1].
Tigatuzumab (CS-1008) is a humanized IgG1 monoclonal antibody targets death receptor 5 (DR5). Tigatuzumab induces cell Apoptosis of cancer cells and inhibits tumor growth in vivo. Tigatuzumab can be used for the research of cancer[1].
Raltitrexed is an antimetabolite drug used in chemotherapy, acting by inhibiting thymidylate synthase.
Vin-C01 is a potent pancreatic β-cells protective agent with an EC50 of 0.22 µM. Vin-C01 effectively promotes β-cell survival and protects β-cells from STZ-induced apoptosis. Vin-C01 can be used for type 2 diabetes mellitus research[1].
ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-turmerone ((+)-ar-Turmerone) activates apoptotic protein in human lymphoma U937 cells[3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation and constitutes a promising therapeutic agent for various neurologic disorders[4][5].
L-threo-PPMP is a GlcT (UDP-Glc: Ceramide β1,1glucosyltransferase) inhibitor. L-threo-PPMP inhibits glycosphingolipid biosynthesis and induces apoptosis. L-threo-PPMP has anti-cancer activity[1].
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].
Nauclefine is an indole alkaloid isolated from Nauclea officinalis. Nauclefine acts as a PDE3A modulator to induce cancer cell apoptosis through a PDE3A-SLFN12-dependent death pathway[1].
FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer[1][2].
Mliademetan is a specific MDM2 inhibitor, a pharmaceutical composition for use in treating acute myeloid leukemia (AML).
10058-F4 is a c-Myc inhibitor that prevents c-Myc-Max dimerization and transactivation of c-Myc target gene expression.
HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma[1].
RIPK2 inhibitor 1 is a novel potent, selective RIPK2 inhibitor with IC50 of 5-10 nM; potently inhibits the proliferation of cancer cells by > 70% and also inhibits NF-κB activity.
FINO2 is a potent ferroptosis inducer. FINO2 inhibits GPX4 activity. FINO2 is a stable oxidant that oxidizes ferrous iron and stable at varying pH levels. FINO2 causes widespread lipid peroxidation[1].
Agelastatin A ((-)-Agelastatin A; AglA), a tetracyclic alkaloid isolated from the sponge Agelas dendromorpha, induces apoptosis and arrests cells in the G2/M phase of the cell cycle, exhibiting antitumor activity[1].
L-Cystine-d4 is the deuterium labeled L-Cystine. L-Cystine is an amino acid and intracellular thiol, which plays a critical role in the regulation of cellular processes.
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine[1]. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2][3][4].
(±)-Trolline ((±)-Oleracein E), an isoquinoline alkaloid, exhibits antibacterial activity against respiratory bacteria and antiviral activity against influenza virus A and B. (±)-Trolline significantly induces HSC apoptosis. (±)-Trolline can be used for the research of liver fibrosis[1].
Telekin is an eucalyptus-type sesquiterpene lactone compound found in Carpesium divaricatum. Telekin can activate mitochondria-mediated cell apoptosis and has anticancer activity[1].
RIPK3-IN-2 is a RIP3 inhibitor. RIPK3-IN-2 can be used in diseases caused by or associate with activated necrotic pathways research[1].
PTG-0861 (JG-265) is a novel potent, selective HDAC6 inhibitor with IC50 of 5.92 nM, >36-fold selectivity over other HDACs.PTG-0861 (JG-265) displays HDAC6 cellular target engagement with EC50 of 0.59 uM (ELISA), has in vitro and cellular selectivity superior to HDAC6-selective inhibitor citarinostat (ACY-241).PTG-0861 (JG-265) demonstrates potency against several blood cancer cell lines (e.g. MV4-11, MM1S), whilst showing limited cytotoxicity against non-malignant cells and CD-1 mice.PTG-0861 (JG-265) exihibits promising in vitro pharmacokinetics achieved with good safety profile in cells and in vivo.