Tubulysin I is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
Cantrixil (TRX-E-002-1), an active enantiomer of TRX-E-002, is a second-generation super-benzopyran (SBP) compound. Cantrixil increases phosphorylated c-Jun levels resulting in caspase-mediated apoptosis in ovarian cancer cells. Cantrixil has potent pan anti-cancer activity against a broad range of cancer phenotypes[1][2].
Oenothein B is a dimeric macrocyclic ellagitannin and has widely pharmacological activities, including antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties. Oenothein B is a potent and specific inhibitor of poly(ADP-ribose) glycohydrolase[1][2].
Z-LEVD-FMK is a cell-permeable caspase-4 inhibitor. Z-LEVD-FMK blocks ER stress-induced apoptosis in cancer cells[1].
Thonningianin A, an ellagitannin, is isolated from the methanolic extract of the African medicinal herb, Thonningia sanguinea. The antioxidant properties of Th A involve radical scavenging, anti-superoxide formation and metal chelation. Anti-cancer activities[1][2].
5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner[1].
Girinimbine (Girinimbin) is a carbazole alkaloid with a variety of biological effects. Girinimbine can induce apoptosis, and has antitrypanosomal, antiplatelet activity, antibacterial activity, anti-inflammatory, antioxidant and antitumor activities[1][2][3].
FAK-IN-5 (Compound 8l) is a FAK signaling inhibitor. FAK-IN-5 induces cell apoptosis and autophagy[1].
PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].
Iodoacetyl-LC-biotin is a biotinylated electrophile probe that can be used to investigate the scope and characteristics of protein covalent binding to subcellular proteomes[1][2].
MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively[1]. MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells[1].
Oxythiamine (Hydroxythiamine) chloride hydrochloride, an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine chloride hydrochloride is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine chloride hydrochloride inhibits cancer cell apoptosis and inhibits cell proliferation[1][2][3].
(S)-SW IV-52 hydrochloride is a small molecule that can induce apoptosis in ovarian cancer. (S)-SW IV-52 hydrochloride has minimal single-agent activity at concentrations up to 200 μM[1].
Cannflavin A can be isolated from Cannabis sativa L. Cannflavin A has anti-cancer, neuroprotective and anti-inflammatory activity. Cannflavin A inhibits Aβ1-42 aggregation. Cannflavin A also inhibits kynurenine-3-monooxygenase (KMO). Cannflavin A activates apoptosis via caspase-3 cleavage[1][2][3][4].
Antitumor agent-80 (compound 11) is an orally active and potent antitumor agent. Antitumor agent-80 induces apoptosis in tumor cells[1].
(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells[1].
β-Carotene-d10 (Provitamin A-d1) is the deuterium labeled β-Carotene. β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities[1][2][3][4][5].
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, which is designed from Brigatinib, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib[1].
MMRi62, a Ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce Autophagy. MMRi62 inducesFerroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12[1][2].
Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3].
(E)-[6]-Dehydroparadol, extracted from patent US 9272994, compound M15, shows growth inhibition and induction of apoptosis against human cancer cells with IC50 values of 43.02 μM in HCT-116 cell and 41.59 μM in H-1299 cell, respectively.
Ferruginol ((+)-Ferruginol), a natural diterpenoid, is an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). Ferruginol inhibits the growth of thyroid cancer cells through the induction of mitochondrial Apoptosis. Ferruginol has antitumor, cardioprotective, antioxidant, gastroprotective, and neuroprotective activities[1][2][3].
Sophoridine is a quinolizidine alkaloid isolated from leafs of Leguminous plant Sophora alopecuroides.L. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor drug candidate for pancreatic cancer with well-tolerated toxicity[1].
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3[1].
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma[1].
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells[1].
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM)[1].Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis[1].Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo[1].
Karanjin is a major active furanoflavonol constituent of Fordia cauliflora. Karanjin induces GLUT4 translocation in skeletal muscle cells by increasing AMPK activity. Karanjin can induce cancer cell death through cell cycle arrest and enhance apoptosis[1][2].
PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.
TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange[1].