AK 295 (CX 295) is a calpain inhibitor that inhibits apoptosis through a calpain-dependent pathway. AK 295 improves neurological function in a rat model of spinal cord injury (SCI). AK 295 can be used in the study of neurodegenerative diseases, such as bulbar amyotrophy, stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis[1].
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].
DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
Sodium oleate (Oleic acid sodium) is an abundant monounsaturated fatty acid sodium[1]. Sodium oleate is a Na+/K+ ATPase activator[2].
RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.
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].
BCP-T.A, a tunable heterocyclic electrophile, is a potent ferroptosis inducer by binding to GPX4[1].
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].
TP-030-1 is an inhibitor of RIPK1. TP-030-1 inhibits hRIPK1 with a Ki value of 3.9 nM and inhibits mRIPK1 with an IC50 value of 4.2 μM. TP-030-1 can be used for the research of inflammatory diseases and neurodegenerative diseases[1].
Ac-AAVALLPAVLLALLAP-DEVD-CHO (DEVD-CHO-CPP 32) is a potent and reversible caspase-3 inhibitor[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].
RIPK1-IN-16 is an orally active and potent inhibitor of RIPK1. RIPK1-IN-16 inhibits excessive inflammation by blocking RIPK1-mediated necroptosis in vivo. RIPK1-IN-16 protects mouse from TNF-induced systemic inflammatory response syndrome and sepsis[1].
LLP-3 is a potent Survivin inhibitor that disrupts the Survivin-Ran interaction in cancer cells. LLP-3 can be used in the research of Glioblastoma multiforme (GBM)[1].
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].
N,O-Didansyl-L-tyrosine cyclohexylammonium is a potent selective thymidylate synthase (TS) inhibitor，acts on TS of Escherichia coli, Lactobacillus casei and human with the IC50 values of 5.0, 3.4 and 119 μM, respectively[1].