Angophorol is a flavonone compound. Angophorol exerts potential anticancer activity through growth inhibition and apoptosis in K562 cells[1].
Mps-BAY2a is a monopolar spindle 1 (MPS1) inhibitor with an IC50 of 1 nM against human MPS1. Mps-BAY2a induces mitotic aberrations and apoptosis in cancer cells[1].
Gefitinib (ZD1839) is a EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
Meloxicam D4 is deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively[1].
Apoptosis Activator 2 is a potent apoptosis activator; increases procaspase-9 processing and subsequent caspase-3 activation.IC50 value: 4-9 uM(Leukemia origin cells)[1]Target: Apoptosis activatorin vitro: Apoptosis Activator 2 promotes the cytochrome c-dependent oligomerization of Apaf-1 into the mature apoptosome. Apoptosis Activator 2 exerted a cytostatic effect on the majority of cell lines tested, inhibiting cell growth by 50–100% at 10 μM in 40 of 48 cell lines tested. Apoptosis Activator 2 exerted a cytotoxic effect, reducing the cell numbers by 10–50% and 50–100% in four and eight cell lines, respectively, from the initial levels when tested at 10 μM. At 100 μM Apoptosis Activator 2 exhibited 100% cytotoxicity in virtually all cell lines, an effect that may be due to nonspecific toxicity. Of the cancer cell lines tested in the panel, cell lines of lymphoid origin (CCRF-CEM, MOLT-4, and Jurkat) were quite sensitive to compound 2-induced killing, with IC50 values ranging from 4 to 9 μM [1]. Apoptosis Activator 2 is a potent and selective carboxylesterase inhibitor with Ki of 67/31/65 nM for hiCE/hCE/rCE respectively, also has less inhibition on AChE/BChE with Ki of 48.2/12.6 uM [2].
Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity[1].
AG6033 is a potential novel CRBN modulator. AG6033 suppresses various tumor cells by modulating the interactions between CRBN and various antitumor target proteins. AG6033 can cause GSPT1 and IKZF1 degradation. AG6033 induces CRBN-dependent cytotoxic effect[1].
RIPGBM is a selective inducer of apoptosis in glioblastoma multiforme (GBM) cancer stem cells (CSCs) with an EC50 of ≤500 nM[1].
Pinoresinol is a lignol of plant origin serving for defense in a caterpillar. Pinoresinol drastically sensitizes cancer cells against TNF-related apoptosis-inducing ligand (TRAIL) -induced apoptosis[1][2].
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis[1].
TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrPC) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis[1].
Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis[1][2][3].
12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway[1].12-HETE has both anti-thrombotic and pro-thrombotic effects[2]. 12-HETE is a neuromodulator[3].
Chondroitin sulfate, one of five classes of glycosaminoglycans, has been widely used in the treatment of osteoarthritis. Chondroitin sulfate reduces inflammation mediators and the apoptotic process and is able to reduce protein production of inflammatory cytokines, iNOS and MMPs.
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC)[1].
Ajoene, a garlic-derived compound, is an antithrombotic and antifungal agent. Ajoene inhibits proliferation and induces apoptosis of human leukaemia CD34-negative cells including HL-60, U937, HEL and OCIM-I. Anticancer activities[1][2].
7,8-Dihydroneopterin, an inflammation marker, induces cellular apoptosis in astrocytes and neurons via enhancement of nitric oxide synthase (iNOS) expression. 7,8-Dihydroneopterin can be used in the research of neurodegenerative diseases[1].
(Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1−/−) and Capan-1 (BRCA2−/−) cells with IC50 values below 0.3 nM[1].
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity[1].
2-tert-Butyl-1,4-benzoquinone is an electrophilic metabolite of butylated hydroxyanisole and an oxidation product of 2-tert-butylhydroquinone[1].
Arylquin 1, a prostate-apoptosis-response-4 (Par-4) secretagogue, targets vimentin to induce Par-4 secretion. Arylquin 1 induces non-apoptotic cell death in cancer cells through the induction of lysosomal membrane permeabilization (LMP)[1].
PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis[1].
Oxysophoridine (Sophoridine N-oxide) is a bioactive alkaloid extracted from the Sophora alopecuroides Linn. Oxysophoridine (Sophoridine N-oxide) shows anti inflammatory, anti oxidative stress and anti apoptosis effects[1][2].
FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research[1][2][3][4].
Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects[1].
Phytohemagglutinin (PHA) is a lectin, obtained from the red kidney bean that binds to the membranes of T-cells, stimulates metabolic activity, cell division, and involves inflammatory pathways. Phytohemagglutinin (PHA) induces apoptosis via increasing proapoptotic protein Bax and activating caspases-3[1][2][3].
Rotundic acid, a triterpenoid obtained from I. rotunda, induces DNA damage and cell apoptosis in hepatocellular carcinoma through AKT/mTOR and MAPK Pathways. Rotundic acid possesses anti-inflammatory and cardio-protective abilities[1].
Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis[1].
TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity[1].