Apoptosis Inducers

Activation and Inhibition of Apoptosis
Several mechanisms have been identified in mammalian cells for the induction of apoptosis. These mechanisms include factors that lead to perturbation of the mitochondria leading to leakage of cytochrome c or factors that directly activate members of the death receptor family. Fas is a member of the tumor necrosis factor (TNF) receptor superfamily, a family of transmembrane receptors that include neurotrophin receptor (p75NTR), TNF-R1, and a variety of other cell surface receptors. Fas Ligand (Fas L) transmits signals to Fas on a target cell by inducing trimerization of Fas. Activation of Fas causes the recruitment of Fas-associated protein with death domain (FADD) via interactions between the death domain of Fas and FADD and is followed by pro-caspase-8 binding to FADD via interactions between the death effector domains (DED) of FADD and pro-caspase-8 leading to the activation of caspase-8. Activation of caspase-8 leads to the activation of other caspases, in effect beginning a caspase cascade that ultimately leads to apoptosis. Caspase-8 activation can also activate Bid, leading to activation of the apoptotic program. Fas-induced apoptosis can be effectively blocked at several stages by either FLICE-inhibitory protein (FLIP), by Bcl-2, or by the cytokine response modifier A (CrmA). In addition, activation of caspase-3 by caspase-9 can be blocked by inhibitor of apoptosis proteins (IAPs). Moreover, the protein kinase, Akt, can be activated by various growth factors and its activity can be blocked by PTEN. Akt functions to promote cell survival through two distinct pathways. Akt inhibits apoptosis by phosphorylating the Bcl-2 family member Bad, which then interacts with 14-3-3 and dissociates from Bcl-xL allowing for cell survival. Alternatively, Akt activates IKK-α that ultimately leads to NF-κB activation and cell survival. Proapoptotic Bcl-2 family members, such as Bax and Bak can promote mitochondrial permeability, while Bcl-2 can inhibit their effects. Upon mitochondrial permeability, apoptogenic factors are released from the mitochondrial inter-membrane space and leak into the cytosol. One factor is cytochrome c, which induces the liberation of protease activators (caspases) that ultimately lead to apoptosis through nuclear damage (DNA fragmentation, DNA mutations). In addition, Smac/Diablo is released and can block IAP inhibition of caspase activity. Mitochondrial permeability is also related to the increased generation of reactive oxygen species (ROS), which plays a role in the degradation phase of apoptosis (i.e. plasma membrane alterations).
Caspase Independent Apoptosis

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A8476 17-(Allylamino)-17-demethoxygeldanamycin ≥98% (HPLC), solid Potent inhibitor of heat shock protein 90 (Hsp90). 17-AAG is a less toxic analog than geldanamycin. It induces apoptosis and displays antitumor effects. 17-AAG inhibits the activity of oncogenic proteins such as N-ras, Ki-ras, c-Akt, and p185erB2.
 DMSO: soluble
methanol: soluble
    • A3105 2-Amino-N-quinolin-8-yl-benzenesulfonamide ≥98% (HPLC), solid Inhibitor of cell cycle at G2 phase; apoptosis inducer.
    		 DMSO: soluble22 mg/mL
    H2O: insoluble
    • SML0256 2OHOA ≥98% (HPLC) 2OHOA induces cell cycle arrest and apoptosis in several cancer cell lines, including glioma, leukemia, breast and colon cancer lines. 2OHOA increases sphingomyelin (SM) levels in the membranes of tumor cells, which typically display decreased SM membrane content, and remodeled membranes, compared with normal cells. The compound has no effect on SM levels in non-cancer cells.
    		 DMSO: >20 mg/mL
    • SML0404 6,8-Bis(benzylthio)-octanoic acid ≥98% (HPLC) CPI-613 is an E1α pyruvate dehydrogenase (PDH) modulator that prevents cancer cells from metabolizing glucose for energy. CPI-613 has been granted orphan drug status by the US FDA for pancreatic cancer.
    		 DMSO: soluble15 mg/mL (clear solution)
    • SML0433   AT101 ≥98% (HPLC) New AT101 [R-(-)-enantiomer of gossypol] is an orally available and well-tolerated natural BH3-mimetic that activates Bax and also induces mitochondrial Smac release. AT101 has shown anti-tumor activity as a single agent and in combination with standard anticancer drugs in a variety of tumor models. AT101 induced apoptosis in chemoresistant ovarian cancer cells.
    		 DMSO: soluble15 mg/mL, clear
    • A4233 Ara-G hydrate ≥98% (HPLC), solid Ara-G is an inducer of apoptosis; inhibitor of DNA synthesis; antineoplastic; and antimetabolite. Ara-G is converted by cellular kinases to the active 5′-triphosphate, Ara-GTP. Incorporation of Ara-GTP into DNA leads to inhibition of DNA synthesis and apoptosis.
    		 DMSO: >10 mg/mL
    H2O: insoluble
    • SRP5164 BAD, GST tagged human recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution    
    • SML0641   BAM7 ≥98% (HPLC) New BAM7 is a selective activator of BAX, a proapoptotic member of the BCL-2 protein family. BAM7 binds directly to the BAX trigger site, a distinct BH3 binding site that regulates BAX activation, inducing BAX oligomerization, which enables the release of apoptogenic factors that result in cell death. BAM7 is selective for this previously unknown BH3-binding groove on the N-terminal face of BAX.
    		 DMSO: soluble2 mg/mL, clear (warmed)
    • SRP5166 BAX, GST tagged human recombinant, expressed in E. coli, ≥70% (SDS-PAGE), buffered aqueous glycerol solution    
    • B8809 BH3I-1 ≥97% (HPLC), powder, yellow BH3I-1is a synthetic cell permeable Bcl-xL antagonist; apoptosis inducer.
    		 DMSO: soluble >10 mg/mL
    H2O: insoluble
    • SRP5168 BID, GST tagged human recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution    
    • SML0140 BV02 ≥98% (HPLC) BV02 is an inhibitor of the 14-3-3 scaffolding proteins docking site. BV02 promotes the apoptotic death of cells expressing either wt Bcr-Abl construct or T315I mutation. It induces apoptosis by c-Abl release from 14-3-3? and re-location to nuclear compartment and at mitochondrial membranes.
    		 DMSO: >5 mg/mL
    • B5437 Bendamustine hydrochloride hydrate ≥98% (HPLC) Bendamustine hydrochloride is a DNA-alkylator with a distinct pattern of activity. Bendamustine activates DNA-damage stress response and apoptosis; inhibits mitotic checkpoints; and induces mitotic catastrophe.
    		 H2O: >30 mg/mL
    • B3061 Borrelidin from Streptomyces parvulus, ≥98% (HPLC) Borrelidin is a potent angiogenesis inhibitor that induces apoptosis in capillary tube-forming cells. Also displays antimalarial activity against drug-resistant Plasmodia. Antimicrobial and selective threonyl t-RNA synthetase inhibitor.
    		 DMSO: soluble1 mg/mL
    methanol: soluble1 mg/mL
    • B1936 Borrelidin from Streptomyces sp., ≥95% (HPLC), lyophilized powder Borrelidin is a potent angiogenesis inhibitor that induces apoptosis in capillary tube-forming cells. Also displays antimalarial activity against drug-resistant Plasmodia. Antimicrobial and selective threonyl t-RNA synthetase inhibitor.
    		 DMF: soluble
    DMSO: soluble
    ethanol: soluble
    ethyl acetate: soluble
    methanol: soluble
    • B5936 Brefeldin A from Penicillium brefeldianum, Ready Made Solution, 10 mg/mL in DMSO, 0.2 μm filtered Brefeldin A (BFA) is a fungal metabolite which disrupts the structure and function of the Golgi apparatus by inhibiting transport of proteins from ER to Golgi and inducing retrograde protein transport from the Golgi apparatus to the endoplasmic reticulum. 1 BFA is an activator of the sphingomyelin cycle. Brefeldin A-mediated apoptosis has been observed in human tumor cells.
    Brefeldin A (BFA) is a fungal metabolite which disrupts the structure and function of the Golgi apparatus. BFA is an activator of the sphingomyelin cycle. Brefeldin A-mediated apoptosis has been observed in human tumor cells.
    		  
    • B0261 Bufalin    
    • C9369 CCT007093 ≥98% (HPLC), powder, yellow CCT007093 is an effective PPM1D inhibitor that selectively reduces viability of human tumour cell lines.
    		DMSO: >3 mg/mL
    • C5865 CD437 ≥98% (HPLC), solid CD437 is a retinoic acid receptor (RAR)γ-selective agonist, γ-selective retinoid; potent inducer of apoptosis.
    		 DMSO: >10 mg/mL
    H2O: insoluble
    • C1244 CHM-1 hydrate ≥99% (HPLC), solid CHM-1 possess antimitotic antitumor activity. It is a potent and selective antitumor agent in human hepatocellular carcinoma. CHM-1 induces apoptosis, and it binds tubulin and inhibits tubulin polymerization.
    		 DMSO: ≥5 mg/mL
    • C5492 CIL-102 ≥95% (HPLC), solid CIL-102 is a tubulin polymerization inhibitor: apoptosis inducer.
    		 DMSO: soluble12 mg/mL
    • PZ0115 CP-31398 dihydrochloride hydrate ≥98% (HPLC) CP-31398 dihyrochloride hydrate is a p53 stabilizer; apoptosis inducer.
    		 H2O: ≥20 mg/mL
    • C4992 Carboxyatractyloside potassium salt ≥98% (HPLC), from Xanthium sibiricum, solid Carboxyatractyloside is a highly selective inhibitor of cytosolic side-specific mitochondrial ADP/ATP carrier; i.e. adenine nucleotide translocase (ANT); causes stabilization of the c conformation of ANT leading to permeability transition pore (PTP) opening, loss of mitochondrial membrane potential, and apoptosis.
    		 H2O: ≥10 mg/mL
    • SML0096 Cinnabarinic Acid ≥98% (HPLC) Cinnabarinic acid is a kynurenine pathway metabolite of tryptophan, produced by the oxidation of 3-Hydroxyanthranilic acid. Cinnabarinic acid leads to loss of mitochondrial respiration and apoptosis, and has also been shown to be an mGlu4R-specific agonist.
    		 DMSO: ≥4 mg/mL
    • C7744 Combretastatin A4 ≥98% (HPLC), powder Combretastatin A4 is a vascular disrupting agent (VDA) that targets tumor vasculature to inhibit angiogenesis. It inhibits tubulin polymerization at the colchicine-binding site of beta-tubulin. It has antitumor activity by inhibiting AKT function in human gastric cells. The inhibited AKT activation causes decreased cell proliferation, cell cycle arrest, and reduced in vitro migration/invasiveness and in vivo metastatic ability. Combretastatin A4 is a natural stilbenoid phenol.
    		 DMSO: >10 mg/mL
    • SML0417 Costunolide ≥97% (HPLC) Costunolide is a sesquiterpene lactone originally isolated from plants widely used in many herbal medicines. It has a variety of effects. Costunolide is a potent inducer of apoptosis, a potent anti-cancer agent, has anti-inflammatory, anti-viral, anti-fungal, antimycobacterial activity and has been shown to inhibit telomerase activity.
    		 DMSO: soluble10 mg/mL (clear solution)
    • SML0031 DBeQ ≥98% (HPLC) DBeQ is a potent and specific inhibitor of ATPase p97, an integral component of the ubiquitin-fusion degradation (UFD) pathway. DBeQ inhibits the degradation of ubiquitinated proteins, the endoplasmic reticulum-associated degradation pathway, and autophagosome maturation. The compound also potently inhibits cellular proliferation and induces caspase 3/7 activity and apoptosis.
    		 DMSO: ≥20 mg/mL
    • SML0363 DIM-C-pPhtBu ≥96% (HPLC) DIM-C-pPhtBu, similar to other C-DIMs, exhibits a broad range of anticancer and antitumorigenic activities against multiple tumor types. DIM-C-pPhtBu causes apoptotic cell death of KB cells by activation of endoplasmic reticulum stress through induction of CHOP protein that is associated with the apoptosis in human oral cancer cells. Also it appears to induce an autophagic cell death in drug-resistant ER-negative breast tumors.
    		 DMSO: >15 mg/mL
    • D5817 DMXAA ≥98% (HPLC), solid DMXAA is an apoptosis inducer; anti-vascular.
    		 DMSO: soluble >10 mg/mL
    • E5161   Enniatin A1 from Gnomonia errabunda, ≥95% (HPLC) Enniatins are a group of cyclohexadepsipeptide mycotoxins produced by Gnomonia errabuda and several Fusaria species, with phytotoxic, antibiotic, and insecticidal activities. Enniatins function as ionophors by their incorporation into the cellular membrane to form dimeric structures that transport monovalent ions across the membrane (especially the mitochondrial membranes) affecting oxidative phosphorylation uncoupling. It has been demonstrated that enniatins have a cytotoxic effect on human cancer cells. Furthermore, incubation of H4IIE hepatoma cells with enniatins strongly diminished phosphorylation of the ERK (p44/p42).
    		 DMSO: soluble10 mg/mL
    ethanol: soluble10 mg/mL
    methanol: soluble10 mg/mL
    • E9661   Enniatin A from Gnomonia errabunda, ≥95% (HPLC) Enniatins are a group of cyclohexadepsipeptide mycotoxins produced by Gnomonia errabuda and several Fusaria species, with phytotoxic, antibiotic, and insecticidal activities. Enniatins function as ionophors by their incorporation into the cellular membrane to form dimeric structures that transport monovalent ions across the membrane (especially the mitochondrial membranes) affecting oxidative phosphorylation uncoupling. It has been demonstrated that enniatins have a cytotoxic effect on human cancer cells. Furthermore, incubation of H4IIE hepatoma cells with enniatins strongly diminished phosphorylation of the ERK (p44/p42).
    		 DMSO: soluble10 mg/mL
    ethanol: soluble10 mg/mL
    methanol: soluble10 mg/mL
    • E5286   Enniatin B1 from Gnomonia errabunda, ≥95% (HPLC) Enniatins are a group of cyclohexadepsipeptide mycotoxins produced by Gnomonia errabuda and several Fusaria species, with phytotoxic, antibiotic, and insecticidal activities. Enniatins function as ionophors by their incorporation into the cellular membrane to form dimeric structures that transport monovalent ions across the membrane (especially the mitochondrial membranes) affecting oxidative phosphorylation uncoupling. It has been demonstrated that enniatins have a cytotoxic effect on human cancer cells. Furthermore, incubation of H4IIE hepatoma cells with enniatins strongly diminished phosphorylation of the ERK (p44/p42). Enniatins B and B1 inhibit the multi-drug resistance transporter Pdr5p from Saccharomyces cerevisiae, indicating their beneficial potential in cases of drug resistant patients.
    		 DMSO: soluble10 mg/mL
    ethanol: soluble10 mg/mL
    methanol: soluble10 mg/mL
    • E5411   Enniatin B from Gnomonia errabunda, ≥95% (HPLC) Enniatins are a group of cyclohexadepsipeptide mycotoxins produced by Gnomonia errabuda and several Fusaria species, with phytotoxic, antibiotic, and insecticidal activities. Enniatins function as ionophors by their incorporation into the cellular membrane to form dimeric structures that transport monovalent ions across the membrane (especially the mitochondrial membranes) affecting oxidative phosphorylation uncoupling. It has been demonstrated that enniatins have a cytotoxic effect on human cancer cells. Furthermore, incubation of H4IIE hepatoma cells with enniatins strongly diminished phosphorylation of the ERK (p44/p42). Enniatins B and B1 inhibit the multi-drug resistance transporter Pdr5p from Saccharomyces cerevisiae, indicating their beneficial potential in cases of drug resistant patients.
    		 DMSO: soluble10 mg/mL
    ethanol: soluble10 mg/mL
    methanol: soluble10 mg/mL
    • E7781 Erastin ≥98% (HPLC), powder Erastin is an antitumor agent selective for tumor cells bearing oncogenic RAS (i.e. HRAS, KRAS). Erastin produces non-apoptotic tumor cell death by altering mitochondrial voltage-dependent anion channel (VDAC) gating allowing cations to enter mitochondria and leading to release of oxidative species causing oxidative cell death.
    		 DMSO: >10 mg/mL
    • E4660 Eupatorin ≥97% (HPLC) Eupatorin acts as an antiproliferative in cells expressing the CYP1A- family. It induces G2/M block follow by apoptosis in cells expressing the CYP1A- family. It also functions as an anti-inflammatory.
    		 DMSO: >10 mg/mL
    • SRP5180 FADD, His tagged human recombinant, expressed in E. coli, ≥70% (SDS-PAGE), buffered aqueous glycerol solution    
    • F9428 Fluticasone propionate ≥98% (HPLC), powder Fluticasone propionate is a second generation glucocorticoid. Used as an anti-inflammatory agent for asthma. Shown to enhance eosinophil apoptosis in a concentration-dependent manner via the glucocorticoid receptor.
    		 DMSO: ≥10 mg/mL
    • G7923 GO-201 trifluoroacetate salt ≥95% (HPLC) GO-201 is a mucin1 (MUC1) inhibitor that binds to the MUC1-C CQC motif and directly blocks MUC1function, inhibits cell proliferation, and induces necrotic cell death in MUC1-positive cell lines. The mucin 1 (MUC1) oncoprotein is aberrantly expressed at high levels in human carcinomas. MUC1 is heterodimer that consists of NH2-terminal (MUC1-N) and COOH-terminal (MUC1-C) subunits. Overexpression of MUC1 blocks the induction of apoptosis and necrosis in the cellular response to DNA-damaging agents, reactive oxygen species, hypoxia ,and glucose deprivation. GO-201 is an inhibitor of MUC1, which interacts directly with the MUC1-C subunit at its oligomerization domain. The compound inhibits cell proliferation and induces necrotic cell death in of MUC1-positive cell lines ant grafts.
    GO-201 is a mucin1 (MUC1) inhibitor that binds to the MUC1-C CQC motif and directly blocks MUC1function, inhibits cell proliferation, and induces necrotic cell death in MUC1-positive cell lines.
    		 H2O: >1 mg/mL
    • G8171 Gambogic acid ≥95% (HPLC), powder Gambogic acid acts as a caspase activator and apoptosis inducer, which causes an irreversible arrest in the G2/M phase of the cell cycle.
    		 DMSO: ≥10 mg/mL
    H2O: insoluble
    • H8787 HA 14-1 ≥95% (CHN/NMR), powder HA 14-1 is a nonpeptide apoptosis inducer; Bcl-2 antagonist.
    		 DMSO: soluble26 mg/mL
    • H4663 HMBA ≥98% (HPLC), solid Inhibitor of microtubule polymerization1; apoptosis inducer.
    		 DMSO: soluble34 mg/mL
    • I7160 IMS2186 ≥98% (HPLC), solid IMS2186 is an anti-proliferative and anti-angiogenic agent. Apparently IMS2186 blocks the cell cycle at G2 and inhibits the production of PGE2/TNF-α. IMS2186 inhibits cell growth in vitro in tumor cells, non-transformed fibroblasts, and retinal pigment epithelial cells. IMS2186 inhibits angiogenesis (IC50 = 0.1 μM) and cell migration. Intraocular injection of IMS2186 could be a long-lasting effective treatment for CNV (choroidal neovascularization) in AMD (age-related macular degeneration) with a reduction in scarring and related visual loss.
    		 DMSO: >20 mg/mL
    • SML0188 Ikarugamycin ≥98% (HPLC), from Streptomyces sp. Ikarugamycin, an unusual pentacyclic tetramic acid produced by Streptomyces sp., has a potent activity against the protozoan Trichomonas vaginalis with IC50 of 0.3-1.25 μg/mL. Ikarugamycin also demonstrates selective Gram positive antibacterial activity and exhibits anti-ulcer activity possibly through inhibition of Helicobacter. Ikarugamycin-induced inhibition of cholesteryl-ester accumulation reduced uptake of oxidized low-density lipoprotein (LDL) in mouse macrophages J774. Moreover, Ikarugamycin inhibits Nef-induced degradation of CD4 on Human Immunodeficiency Virus type 1 (HIV) infected T cells, thus increasing its half-life and possibly restoring some normal functions lost in the infected cells. Ikarugamycin inhibition of clathrin-coated pit-mediated endocytosis indicates it as a useful agent for studying the process of endocytosis. Ikarugamycin inhibit HL-60 cell proliferation through genotoxicity and apoptosis induction and to activated caspase by induction of intracellular rise in calcium levels and activation of p38 MAP kinase.
    		 DMSO: soluble5 mg/mL (requires heating and sonication)
    chloroform: soluble1 mg/mL (requires heating and sonication)
    methanol: soluble1 mg/mL (requires heating and sonication)
    • I5159 Imiquimod ≥98% (HPLC), solid Imiquimod is a caspase 3 activator, which directly induces procaspase 3 cleavage to active caspase 3. Imiquimod induces apoptosis in vivo in basal cell carcinoma. Its anti-tumor activity is related to the induction of apoptosis. Imiquimod has anti-angiogenic, anti-inflammatory, anti-viral activities. Imiquimod also acts as an immune response modulator inducing the secretion of various cytokines and chemokines.
    		 DMSO: soluble4 mg/mL (warming to 60 °C for 15 minutes)
    H2O: <2 mg/mL
    • SML0623   Iniparib ≥98% (HPLC) New Iniparib (BSI-201) is an antineoplastic originally thought to be a poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. Recent studies indicate Iniparib is not a PARP-1 inhibitor, and its mechanism of action is currently unknown.
    		 DMSO: soluble5 mg/mL, clear
    • SRP4928   Lipocalin-2 human recombinant, expressed in E. coli, ≥95% (SDS-PAGE), ≥95% (HPLC)    
    • SML0040 Lometrexol hydrate ≥95% (HPLC) Glycinamide Ribonucleotide Formyltransferase (GARFTase) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexate is a potent inhibitor of GARFTase, but does not interfere with enzymes involved in the synthesis of folate. Lometrexerol has been tested clinically for the treatment of various cancers as an anti-folate like agent, similar to methotrexate. Treatment with lometrexol rapidly decreases ATP and GTP levels, cell cycle arrest and induces apoptosis. Although depletion of nucleotide pools induces p53 expression, lometrexol is cytotoxic in both wild-type and mutant p53 expressing tumor cells. Lometrexol is cytotoxic in CCRF-CEm leukemia cells with an IC50 of 2.9 nM.
    		DMSO: ≥5 mg/mL
    • SML0521 ML 210 ≥98% (HPLC) ML 210 induces non-apoptotic cell death in tumor cells expressing the RAS oncogene.
    		  
    • M7888 Muristerone A ≥90% Muristerone A is a native phytosteroid known to have insecticidal properties. Induces apoptosis in cell transfected with wild-type Bax and ecdysone-inducible gene expression systems in mammalian cells and transgenic animals.
    		  
    • SML0507 NPC26 ≥98% (HPLC) NPC26 induces mitochondrial fragmentation and cell death in RAS expressing cells, similar to erastin. The effects of NPC26 are independent of ROS scavengers, which can block cell death induced by erastin.
    		 DMSO: soluble2 mg/mL (clear solution, warmed)
    • N9162 Neocarzinostatin from Streptomyces carzinostaticus ≥90% (SDS-PAGE), ~0.5 mg/mL Neocarzinostatin is a protein-small molecule complex composed of an enediyne chromophore tightly bound to a 113 amino acid single chain protein. The complex possesses antiproliferative and antitumor activity. The chromophore is the active compound, which is responsible for DNA cleavage; while the apoprotein stabilizes and regulates the availability of the labile chromophore. NCS chromophore is bound non-covalently in a cleft of the binding protein and is dissociable. Upon addition of a thiol, the chromophore forms a highly reactive biradical species that can induce sequence-specific single and double strand breaks in DNA. Neocarzinostatin inhibits DNA synthesis and possesses antitumor activity in various human and animal tumors. NCS inhibits cellular proliferation by inducing G2 cell cycle arrest and apoptosis in both human papillomavirus (HPV) positive and negative cell lines.
    		  
    • SML0610   Nitidine chloride ≥97% (HPLC) New Nitidine chloride is a natural product with anti-cancer activity. Its mechanism of action likely involves several pathways. Nitidine chloride has been found to inhibit topoisomerase I and topoisomerase II, induce cell apoptosis by activation of the caspase-dependent pathway, suppress c-Src/FAK associated signaling pathways and suppress Janus kinase 2/STAT3 signaling and the expression of STAT3-dependent target genes, including cyclin D1, Bcl-xL, and VEGF. Nitidine chloride has also been found to have anti-malaria activity.
    		 DMSO: soluble1 mg/mL, clear (warmed)
    • N6287 Nutlin-3 ≥98% (HPLC), powder Nutlin-3 is a Mdm2 (mouse double minute 2) antagonist, p53 pathway activator, and apoptosis inducer.
    		 DMSO: soluble20 mg/mL
    H2O: insoluble
    • SML0580   Nutlin-3a ≥98% (HPLC) New Nutlin-3a [(-)-Nutlin] is a more potent diastereoisomer of racemic MDM2 antagonist Nutlin-3. It was called enantiomer-a since it elutes as the first peak from chiral purification of racemic nutlin-3. Nutlin-3a is a potent inhibitor of MDM2 (mouse double minute 2) binding to p53 that induces the expression of p53 regulated genes, and shows potent antiproliferative activity in cells expressing functional p53. Nutlin-3a is 150 times more potent than Nutlin-3b.
    		 DMSO: soluble5 mg/mL, clear
    • K4394 PKF118-310 ≥98% (HPLC), powder PKF118-310 is an antagonist of the Tcf4/b-catenin signaling. The compound disrupts the Tcf4/b-catenin complex and inhibits expression of Tcf4 responsive genes. PKF118-310 inhibits expression of survivin and induces apoptosis in HCC, colon tumor and lymphocytic leukemia cell lines.
    		 DMSO: ≥15 mg/mL
    • P0069 PRIMA-1 ≥98% (HPLC), solid PRIMA-1 is a selective re-activator of mutant p53 activity in tumor cells, and an inducer of apoptosis and inhibitor of growth of human tumors with mutant p53. Mutations in the tumor suppressor p53 take place in >50% tumor cells. PRIMA-1 selectively restores sequence-specific DNA binding and transactivational activity to mutant p53 proteins at μM concentrations. PRIMA-1 works as a re-activator of the apoptotic function of mutant p53 via conformational modulation of function-specific epitopes.
    		 H2O: >10 mg/mL
    • G7548 Penta-O-galloyl-β-D-glucose hydrate ≥96% (HPLC) PGG induces predominantly (caspase dependent) apoptosis in DU145 and LNCaP cells, while inducing autophagy in more resistant PC3 and TRAMP-C2 cells. It appears that PGG targeted signaling downstream of rather than the mTOR itself. Polyphenolic pyranoses were reported (J Biol Chem. 2010, 285 (11), 7892-902) to inhibit the plasminogen activator inhibitor type 1 (PAI-1).
    		 DMSO: ≥20 mg/mL
    • D7446 Phenoxodiol ≥98% (HPLC) Phenoxodiol is a Pan-cancer drug; causes apoptosis via both intrinsic and extrinsic pathways; targets plasma membrane electron transport (PMET).
    		 DMSO: >10 mg/mL
    • P0103   Prodigiosin hydrochloride from Serratia marcescens, ≥98% (HPLC), powder Prodigiosin, a tripyrrole red pigment biosynthesized by Serratia marcescens and other bacteria, exhibits antibacterial, anticancer, cytotoxic, immunosuppressive, and antiproliferative activities.1,2,3 Prodigiosin induces apoptosis in hematopoietic cancer cells and cells derived from other human cancers, including gastric and colon with no marked toxicity in nonmalignant cell lines.2,4,5 Morphological analysis of prodigiosin-treated cells demonstrated that prodigiosin induces cell shrinkage, chromatin condensation, reorganization of actin microfilament architecture, and detachment of cells from the cell culture substrate.6 Different targets and mechanisms of action are described for prodigiosin, including induction of single- and double-strand DNA breaks, modulation of pH, regulation of mitogen-activated protein kinase, and inhibition of cell cycle progression.5
    		 DMSO: soluble
    H2O: insoluble
    acetonitrile: soluble
    chloroform: soluble
    methanol: soluble
    • P1499 Pterostilbene ≥97% (HPLC), solid Antioxidant, antiproliferative, apoptosis inducer, antihyperglycemic, antidiabetic.
    		 DMSO: >20 mg/mL
    H2O: insoluble
    • R9156 Raltitrexed monohydrate ≥98% (HPLC), solid Raltitrexed is a folate-based inhibitor of thymidylate synthase (TS) that is rapidly and extensively metabolized to its more potent polyglutamate derivatives. By inhibiting the formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.
    		 DMSO: ≥40 mg/mL
    H2O: ≥10 mg/mL
    • R5030 Ridaifen-B ≥98% (HPLC), white solid Ridaifen-B (RID-B) is a novel tamoxifen (TAM) analog that significantly augments apoptosis-inducing effect of TAM in estrogen receptor (ER)-negatives cells. Ridaifen-B induces mitochondria-involved apoptosis in Jurkat cells, as evidenced by chromatin-condensed cells as well as downstream activation of caspases (caspase-3, -8 and -9) in a dose- and time-dependent manner. At 4 hours of incubation, IC50 for RID-B is 4 muM (30 muM for TAM). And at prolonged treatment of 48 hours, IC50 for RID-B is 0.1 muM.1 In a related report2 on the global anti-tumor activity, RID-B strongly inhibits 39 human cancer cells (JFCR 39), both ER-+ or ER-- at concentrations of equal or less than 1muM (e.g., at 0.38muM for SF-539 [central nervous system], at 0.58muM for HT-29 [colon], at 0.20muM for DMS114 [lung], at 0.21muM for LOX-IMVI [melanoma], and at 0.23muM for MKN74 [stomach]. The binding protein of RID-B that exerts the apoptosis events is currently under investigation.
    		 DMSO: ≥13 mg/mL
    H2O: insoluble
    • R3530   Rifabutin >98% (HPLC), powder Rifabutin is an antibiotic; antitumor. Rifabutin interferes with HSP-90 molecular chaperone, enhances ubiquitination and protein degradation, and inactivates bacterial RNA polymerase.
    		 DMSO: >5 mg/mL
    • S7451 SJ-172550 ≥98% (HPLC) SJ-17255 is a MDMX inhibitor. Similarly to MDM2, MDMX regulates p53. But in contrast to MDM2, MDMX appears to directly regulate p53 transcription. SJ-172550 is a first small-molecule inhibitor of MDMX with a low micromolar binding constant. It appears that SJ-172550 is binding to the p53-binding pocket of MDMX, thus liberating p53 to induce apoptosis.
    		 DMSO: ≥30 mg/mL
    • S7448 STF-62247 ≥98% (HPLC), solid STF-62247 is a selective inducer of autophagy in VHL-deficient renal cell carcinoma cells.
    		 DMSO: soluble26 mg/mL
    H2O: insoluble
    • T7329 Taurolidine >97% (NMR), powder Taurolidine is a broad spectrum antibiotic with antineoplastic activity, which induces apoptosis and decreases tumor cell proliferation. Taurolidine has been used with TNF-related-apoptosis-inducing ligand (TRAIL) to characterize synergistic responses in many apoptosis related signaling-proteins. Tauroline is also being used as a tool to study the various mechanisms of apoptosis and necrosis.
    		 DMSO: >20 mg/mL
    • T2577 Temozolomide ≥98% (HPLC) Temozolomide is a DNA methylating agent and drug resistance-modifying agent; anti-tumor and anti-angiogenic. Temozolomide induces G2/M arrest and apoptosis through adduction of a methyl group to O6 position of guanine in genomic DNA and functional inactivation of DNA repair protein O(6)-alkylguanine DNA alkyltransferase (AGT) in base excision repair (BER) pathway.
    		 DMSO: >20 mg/mL
    H2O: insoluble
    • SML0552 Tirapazamine ≥98% (HPLC) New Under hypoxic conditions, tirapazamine is a potent cytotoxic agent that induces apoptosis by inducing breaks in single and double stranded DNA, as well as chromosomal breaks. The compound sensitizes cells to other ionizing radiation and other cytotoxic agents like cisplatin.
    		 DMSO: soluble10 mg/mL, clear
    • SML0367 VK3-OCH3 ≥98% (HPLC) VK3-OCH3 is an analog of Vitamin K3 (Menadione) with potent antitumor activity. It has been shown to induce G2/M arrest and apoptosis in neuroblastoma cells with much less cytotoxicity towards normal cells. VK3-OCH3 is believed to act through up-regulation of heme oxygenase (HO)-1.
    		 DMSO: soluble10 mg/mL (clear solution)
    • V9389   Violacein from Janthinobacterium lividum >98% (violacein (minimum 85% violacein) and deoxyviolacein, HPLC) Violacein, a violet pigment, is an indole derivative produced by various bacterial strains such as Chromobacterium violaceum, Janthinobacterium lividum, Chromobacterium lividum, and Pseudoalteromonas luteoviolacea. Violacein is a member of a novel class of cytotoxic drugs, which mediate apoptosis.1 Violacein exhibits antitumoral, antibacterial, antiulcerogenic, antileishmanial, and antiviral activities.2,3,4,5 Violacein and its β-cyclodextrin complexes trigger apoptosis and differentiation in HL60 leukemic cells.2 Violacein cytotoxicity is preceded by activation of caspase 8, transcription of NF-κB target genes, and p38-MAPK activation resembling TNF-α signal transduction.1
    		 H2O: insoluble
    acetone: soluble
    ethanol: soluble
    methanol: soluble
    • Z3902 Zerumbone ≥98% (HPLC) Zerumbone is a TRAIL-induced apoptosis potentiator. It potentiates TRAIL-induced apoptosis through the up-regulation of DR4 and DR5 expression and the down-regulation of cFLIP. Zerumbone has very little or no cytotoxic effect on the normal human endothelial cells and dermal fibroblasts. Zerumbone is a sesquiterpene isolated from in Zingiber zerumbet Smith (wild ginger).
    		DMSO: ≥10 mg/mL
    • SRP3199   gAcrp30 from mouse recombinant, expressed in E. coli, ≥98% (SDS-PAGE), ≥98% (HPLC), cell culture tested gAcrp30 is a naturally occurring globular protein, obtained by proteolytic processing of adiponectin. Recombinant murine gAcrp30 is a 16.6 kDa protein consisting of 145 amino acid residues.
    		  
    • SRP3046   gAcrp30/Adipolean human recombinant, expressed in E. coli, ≥98% (SDS-PAGE), ≥98% (HPLC), cell culture tested gAcrp30 is a naturally occurring globular protein, obtained by proteolytic processing of adiponectin. Recombinant human gAcrp30/Adipolean is a 16.6 kDa protein consisting of 145 amino acid residues.
    		  
    • SRP3047   gAcrp30/Adipolean variant human recombinant, expressed in E. coli, ≥98% (SDS-PAGE), ≥98% (HPLC), cell culture tested The gAcrp30 variant is a naturally occurring globular protein, obtained by proteolytic processing of adiponectin. AdipoR2 is predominantly expressed in the liver. This naturally occurring variant of human gAcrp30/Adipolean is an 18.1 kDa protein, containing 14 amino acids extra at the N-terminus of human gAcrp30/Adipolean.