N-Methylhemeanthidine chloride is an amaryllidaceae alkaloid isolated from Zephyranthes candida. N-Methylhemeanthidine chloride has antitumor activity and can inhibit cancer cell proliferation by down-regulating < a href=" " class="link-product" target="_blank">AKT activation, mediating cell cycle arrest and inducing < a href=" " class="link-product" target="_blank">apoptosis[1].
Cearoin, isolated from Dalbergia odorifera, increases autophagy and apoptosis through the production of ROS and the activation of ERK[1].
Amiloride-15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride[1]. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC[2]) and urokinase-type plasminogen activator receptor (uTPA[3]). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2[4]) channel.
Citatuzumab bogatox (VB6-845) is recombinant immunotoxin that composed of Fab fragment of humanized antibody targeting EpCAM and a modified cytotoxin bouganin. Citatuzumab bogatox binds to and selectively induces Apoptosis in EpCAM-positive cell lines and shows good activity in EpCAM-positive human tumour xenograft models[1][2][3].
Illudin S is a sesquiterpene toxin with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities[1][2][3].
Vincristine-d3 (Leurocristine-d3) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1][2].
Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly[1][2].
iMAC2 is a potent MAC inhibitor with an IC50 of 28 nM and an LD50 of 15000 nM. iMAC2 shows anti-apoptotic effect. iMAC2 blocks cytochrome c release[1].
Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor for the treatment of osteoarthritis. Licofelone (ML-3000) exerts anti-inflammatory and anti-proliferative effects. Licofelone (ML-3000) induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[1][2].
GGTI 2417 is the methyl ester prodrug of GGTI-2418, a highly potent, competitive, and selective inhibitor of GGTase I; exhibits potent inhibitory activity against Rap1 geranylgeranylation with IC50 of 400 nM; increases p27 protein levels and induces accumulation in the G0/G1 phase as well as apoptotic cell death in breast cancer cells, and prevents the degradation of nuclear p27.
Triphen diol is a phenol diol derivative, which has excellent anticancer activity against pancreatic cancer and cholangiocarcinoma, and can induce pancreatic cell apoptosis through two mechanisms, caspase-mediated and caspase-independent[1].
NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.Target: nucleophosminin vitro: NSC348884 is a putative nucleophosmin small molecular inhibitor that disrupts a defined hydrophobic pocket required for oligomerization. NSC348884 disrupts nucleophosmin oligomer formation by native polyacrylamide gel electrophoresis assay. NSC348884 upregulates p53. NSC348884 induces apoptosis.[1]
Tubulysin F 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 F is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
Tiron is a non-toxic chelator of a variety of metals. Tiron is cell permeable analog of vitamin E and function as hydroxyl radical and superoxide scavenger. Tiron is an orally active antioxidant. Tiron can be used to alleviate acute metal overload in animals[1][2][3].
α-NETA is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM. α-NETA is a potent chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM). α-NETA has anti-cancer activity[1][2].
4-Hydroxybenzyl alcohol is a phenolic compound widely distributed in various kinds of plants. Anti-inflammatory, anti-oxidant, anti-nociceptive activity. Neuroprotective effect. Inhibitor of tumor angiogenesis and growth[1][2][3][4].
MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity[1][2].
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively[1].
Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research[1].
ST1074 is a dual CerS2/CerS4 inhibitor that induces apoptosis. ST1074 can be used in cancer research[1].
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts[1][2].
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity[1].
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell Apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer[1].
HS-1793 is a resveratrol analogue with antitumor activities in a variety of cancer cell lines[1]. HS-1793 induces cell apoptosis[2].
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase[1].
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2[1].
Nonactin is a naturally occurring macrotetrolide antibiotic from Streptomyces griseus. Nonactin acts as an ionophore for monovalent cations, including K+, and NH4+[1]. Nonactin is able to uncouple the oxidative phosphorylation of mitochondria. Nonactin selectively induces apoptosis in cell lines harboring active mutant β-catenin[2]. Nonactin inhibits the surface expression of endogenous HSP60[3].
Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis[1].
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor[1].
Lumichrome, a photodegradation product of Riboflavin, is an endogenous compound in humans. Lumichrome inhibits human lung cancer cell growth and induces apoptosis via a p53-dependent mechanism[1][2].