PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε)[1][2].
Monomethyl auristatin E (MMAE) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
Epimedokoreanin B is a natural flavonoid with anticancer, anti-inflammatory and antibacterial effects. Epimedokoreanin B inhibits the growth of lung cancer cells through endoplasmic reticulum stress-mediated Apoptosis accompanied by autophagosome accumulation. Epimedokoreanin B is an anti-periodontitis agent that inhibits gingipains and Porphyromonas gingivalis growth and biofilm formation[1][2][3].
Sparfosic acid is a DNA antimetabolite agent and a potent inhibitor of aspartate transcarbamoyl transferase. Sparfosic acid has anti-tumor activity. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis[1][2].
Methylophiopogonanone A, a major homoisoflavonoid in Ophiopogon japonicas, has both anti-oxidative and anti-inflammatory properties[1].
IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC)[1].
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo[1].
Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml [2]. Pogostone induces cell apoptosis and autophagy[2].
Sodium oleate (Oleic acid sodium) is an abundant monounsaturated fatty acid sodium[1]. Sodium oleate is a Na+/K+ ATPase activator[2].
Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment[1][2].
5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis[1][2][3][4][5].
Citronellyl acetate is a monoterpene product of the secondary metabolism of plants, with antinociceptive activity. Citronellyl acetate exhibits pro-apoptotic activity in human hepatoma cells. Citronellyl acetate shows fungicidal, larvicidal, bactericidal and repelling/insecticidal effects[1].
HP661 is an orally available oxidative phosphorylation (OXPHOS) inhibitor that effectively blocks the activity of mitochondrial complex I and reduces the production of the reactive oxygen species. HP661 can abrogate the growth of high OXPHOS-dependent tumors, conquer high OXPHOS-mediated drug resistance, and can induce cell apoptosis. And HP661 can be used for anti-tumor research[1].
Tubulin polymerization-IN-31 (Compound 4c) is a tubulin polymerization inhibitor with an IC50 of 3.64 μM. Tubulin polymerization-IN-31 induces cancer cell apoptosis and shows antitumor activity[1].
Delphinidin 3-rutinoside chloride (Delphinidin 3-O-rutinoside chloride) is an active anthocyanin found in bilberry extract. Delphinidin 3-rutinoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL)[1]. Delphinidin 3-rutinoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC50 of 2.3 μM[2].
Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis[1][2][3].
Asiatic acid, a pentacyclic triterpene found in Centella asiatica, induces apoptosis in melanoma cells. Asiatic acid can be used to treat skin cancer[1]. Asiatic acid also has anti-inflammatory activities[2].
Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells[1][2].
CYD-2-11 is a novel potent, selective Bax agonist that targets the structural pocket proximal to S184 in the C-terminal region of Bax (Ki=34.1 nM); shows no affinity for other Bcl-2 family members; directly activates Bax proapoptotic activity by inducing a conformational change enabling formation of Bax homooligomers in mitochondrial membranes; suppresses malignant growth without evident significant toxicity to normal tissues in mutant KRAS-driven lung cancer models; displays strong synergistic activity and overcomes rapalog resistance combined with RAD001.
Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities[1][2][3][4][5]. Demethylzeylasteral can significantly alleviates atherosclerosis (AS)[5]. Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways[2].
Minodronic acid-d4 is deuterium labeled Minodronic acid. Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain[1][2].
Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC50s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities[1][2].
SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines[1][2].
Apoptosis inducer 6 (compound 4e) is an anticancer agent with a broad-spectrum anticancer activity. Apoptosis inducer 6 triggers cell death through the induction of apoptosis[1].
S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities[1][2].
Anti-osteoporosis agent-1 (comp 4aa) is a potent replication protein A (RPA) inhibitor (IC50=18 µM) [1].
L-Glutamic acid monosodium hydrate is a nutritional additive and flavoring agent. L-Glutamic acid monosodium hydrate can reduce obesity and induce metabolic disorders associated with oxidative stress. L-Glutamic acid monosodium hydrate induces oxidative stress,DNA damage and apoptosis in the liver and brain tissues of mice[1][2].
ABT-510 acetate is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 acetate also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 acetate can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD)[1][2].
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization[1].
5-Aminolevulinic acid-d2 (hydrochloride) is deuterium labeled 5-Aminolevulinic acid (hydrochloride).