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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SML1533   (±)-Marinopyrrole A ≥95% (HPLC) Marinopyrrole A (Maritoclax) is a potent and selective inhibitor of Bcl-2 family member Mcl-1, originally isolated from marine streptomycetes for its antimicrobial activity against methicillin-resistant Staphylococcus aureus. Marinopyrrole A directly binds to Mcl-1 and targets it for proteasomal degradation. Marinopyrrole A induced apoptosis in Mcl-1-dependent cancer cells and sensitized cancer cells to ABT-737.
DMSO: 20 mg/mL clear
SML0963   (E)-3,4,5,4′-Tetramethoxystilbene ≥98% (HPLC) (E)-3,4,5,4′-Tetramethoxystilbene (DMU 212) is a derivative of resveratrol with anti-angiogenic and anti-tumor properties.
DMSO: 5 mg/mL clear (warmed)
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
SMB00388 2,4,3′,5′-tetramethoxystilbene ≥98% (HPLC) 2,3′,4,5′-Tetramethoxystilbene, also known as TMS, is a selective and competitive inhibitor of cytochrome P450 1B1, an overexpressed enzyme in particular tumors. TMS is also a selective inhibitor of CYP1B1.
 
A3105 2-Amino-N-quinolin-8-yl-benzenesulfonamide ≥98% (HPLC), solid Inhibitor of cell cycle at G2 phase; apoptosis inducer.
DMSO: soluble 22 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: 15 mg/mL (clear solution)
SML0433   AT101 ≥98% (HPLC) 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: 15 mg/mL clear
SML0907 Apoptolidin A Ready Made Solution 1 mg/mL in DMSO Apoptolidin A is a 20-membered macrolide shown to be selectively cytotoxic against several cancer cell lines and noncytotoxic against normal cells. The molecule was originally produced by Nocardiopsis species, and its target site was identified as mitochondrial F0F1-ATPase.
Apoptolidin induces apoptosis selectively in rat glia cells transformed with the adenovirus oncogene E1A. Several minor apoptolidin congeners were isolated, known as Apoptolidins A-D. All apoptolidins were reported to inhibit growth of H292 cancer cells (lung carcinoma) in the submicromolar range. Recently, a stereo-selective synthesis of the Apoptolidin disaccharide was reported.
 
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
SML1263 Arylquin 1 ≥98% (HPLC) Arylquin 1 is a potent secretagogue of the tumor suppressor protein prostate apoptosis response-4 (Par-4), selectively inducing apoptosis in a variety of cancer cells. Arylquin 1 acts by binding to vimentin, displacing Par-4 from vimentin for secretion. Arylquin 1 produced a dose-dependent secretion of Par-4 at nanomolar concentrations.
DMSO: 20 mg/mL clear
SRP5164 BAD, GST tagged human recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution    
SML0641   BAM7 ≥98% (HPLC) 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: 2 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    
BM0018 BMS-906024 ≥98% (HPLC) BMS-906024 is a γ-secretase inhibitor and pan-Notch inhibitor with antineoplastic activity. BMS-906024 is being studied as an anticancer agent and has shown good anti-leukemic activity in a case of early T-cell progenitor acute lymphoblastic leukemia.
DMSO: 20 mg/mL clear
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: 1 mg/mL
methanol: 1 mg/mL
SML1635 Brassinin ≥98% (HPLC) Brassinin is a phytoalexin isolated from cruciferous vegetables that exhibits anticancer, chemopreventive, antiproliferative and antifungal activities. In lung cancer cells, brassinin inhibits constitutive and IL-6-inducible STAT3 signaling through modulation of PIAS-3 and SOCS-3. It appears that brassinin induces apoptosis in PC-3 prostate cancer cells via the suppression of PI3K/Akt/mTOR/S6K1 signaling.
DMSO: 20 mg/mL clear
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. BFA inhibits the transport of sphingomyelin to the surface of mammalian cells. The ester derivatives of BFA exhibit anti-cancer properties.
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.
DMSO: 10 mg/mL
B0261 Bufalin    
SML1827 CCF642 ≥98% (HPLC) CCF642 is a cell-permeable protein disulfide isomerase (PDI) inhibitor that exhibits 100-fold higher potency than PACMA 31 (by di-E-GSSG assay) via an alternative mode of action that most likely involves PDI active-site CGHCK motifs instead of cysteine known to be targeted by PACMA 31. CCF642 displays anti-multiple myeloma (MM) activity both in cultures in vitro (IC50 <1 μM against murine 5TGM1 and nine human MM lines) and in mice in vivo (10 mg/kg, 3X i.p. per wk) without apparent adverse effects to the animals or being cytotoxic to normal bone marrow (NLBM) cells even at concentrations as high as 6.75 μM. Consistent with PDI′s role in ER protein folding process, CCF642 treatment causes acute ER stress accompanied by apoptosis-inducing calcium release in MM cells.
DMSO: 5 mg/mL clear (warmed)
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: 12 mg/mL
PZ0115 CP-31398 dihydrochloride hydrate ≥98% (HPLC) CP-31398 dihyrochloride hydrate is a p53 stabilizer; apoptosis inducer.
H2O: ≥20 mg/mL
SML1016 Camalexin ≥98% (HPLC) Camalexin is a phytoalexin isolated from cruciferous plants that exhibits antibacterial, antifungal, antiproliferative and cancer chemopreventive activities. Apparently, camalexin increases the ROS levels and is more effective in aggressive prostate cancer cells that express high ROS levels. In Arabidopsis thaliana, camalexin and salicylic acid confer resistance to Phytophthora capsici.
DMSO: 20 mg/mL clear
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
SML1269 Cepharanthine ≥95% (HPLC) Cepharanthine is an anti-inflammatory, antiallergic, immunomo- modulatory and antineoplastic alkaloid isolated from Stephania cepharantha Hayata. Cepharanthine is an inhibitor of efflux transporter ABCC10. Also, Cepharanthine binds to central portion of Hsp90 with Kd 15 nM. Recent studies suggest that Cepharanthine inhibits the entry of HIV-1 by reducing plasma membrane fluidity.
DMSO: 10 mg/mL clear
SMB00418 Cepharanthine ≥98% (HPLC) Cepharanthine has anticancer, anti-inflammatory, anti-allergic, immunomodulatory, anti-angiogenic, and apoptosis-inducing activities.
 
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
SML0953   Cirsiliol ≥95% (HPLC) Cirsiliol is a flavonoid that displays anti-inflammatory, anti-oxidant, anti-proliferative, and anti-bacterial activities. Cirsiliol sensitizes non-small cell lung cancer cell lines (NSCLC) to radiation therapy. Cirsiliol inhibits epithelial-mesenchymal transition likely by induction of tumor-suppressive miR-34a, which suppresses Notch-1 expression NSCLC.
DMSO: 10 mg/mL clear
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: 10 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
SML1765 DPBQ ≥98% (HPLC) DPBQ is a potent apoptosis inducer that is specific for high-ploidy cells. It appears that DPBQ induces expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
DMSO: 10 mg/mL clear
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: 10 mg/mL
ethanol: 10 mg/mL
methanol: 10 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: 10 mg/mL
ethanol: 10 mg/mL
methanol: 10 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: 10 mg/mL
ethanol: 10 mg/mL
methanol: 10 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: 10 mg/mL
ethanol: 10 mg/mL
methanol: 10 mg/mL
E7781 Erastin ≥98% (HPLC) Erastin is an antitumor agent selective for tumor cells bearing oncogenic RAS (i.e. HRAS, KRAS). Erastin produces ferroptosis, a 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: 5 mg/mL clear (warmed)
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
SML1131 Fosbretabulin disodium ≥98% (HPLC) Fosbretabulin disodium (Combretastatin A4 phosphate, CA4P) is a potent vascular-disrupting agent (VDA). Fosbretabulin disodium is a prodrug that is converted to combretastatin A (Sigma Cat No. C7744) inside the endothelial cells that line blood vessels, where it binds to tubulin dimers and prevents microtubule polymerization, resulting in mitotic arrest and apoptosis in endothelial cells. Fosbretabulin disodium is a potent anti-cancer agent that exhibits antivascular effects on tumor vasculature, inducing a rapid reduction in tumor blood flow and a concomitant increase of cellular necrosis. Some of its activity is believed to involve interference with vascular endothelial-cadherin signaling in addition to its microtubule-disrupting activity.
H2O: 5 mg/mL clear
G7923 GO-201 trifluoroacetate salt ≥95% (HPLC) GO-201 binds with the cytoplasmic domain of MUC1 (mucin 1) protein, thus preventing the oligomerization of MUC1 protein in cells. In human breast cancer cells, this peptide prevents the transport of MUC1 to nucleus, causes disruption of redox equilibrium and induces DNA damage response. It prevents the interaction between NFκB (nuclear factor) and MUC1, thus, preventing activation of MUC1 by NFκB. GO-201 suppresses the expression of the anti-apoptotic protein Bcl-xL (B-cell lymphoma-extra large). This peptide also inhibits growth and initiates death by necrosis. Studies in nude mice with human breast tumor xenograts, show that the use of GO-201 results in massive necrosis and intensive regression of tumorigenesis.
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: 26 mg/mL
H4663 HMBA ≥98% (HPLC), solid HMBA is an Inhibitor of microtubule polymerization; apoptosis inducer.
DMSO: soluble 34 mg/mL
SML1637 Hexaminolevulinate hydrochloride ≥98% (HPLC) Hexaminolevulinate (HAL) hydrochloride is a hexyl ester of 5-Aminolevulinic acid (ALA), a precursor to porphyrins including the photosensitizer protoporphyrin IX (PPIX). Hexaminolevulinate is more lipophilic than ALA, and is 50–100 times more efficient than ALA at inducing PpIX, which accumulates preferentially in neoplastic cells. Hexaminolevulinate administration followed by light activation has been used for fluorescence cystoscopy to enhance detection of bladder cancer, in particular carcinoma in situ (CIS). Hexaminolevulinate is also being studied for use in cancer photodynamic therapy. Hexaminolevulinate followed by irradiation produced DNA oxidative damage and apoptosis.
H2O: 20 mg/mL clear
SML1903 IMB5046 ≥98% (HPLC) IMB5046 is a microtubule inhibitor that has antitumor activity, overcoming multidrug-resistance. IMB5046 was cytotoxic with an IC50 range of 37 to 426 nM against multiple tumor cell lines, including some that were resistant to colchicine, vincristine and paclitaxel. IMB5046 was also active against human lung tumor xenografts. IMB5046 was found to bind to tubulin at the colchicine site, but with a different binding mode. IMB5046 inhibited tubulin polymerization, and induced G2/M arrest.
DMSO: 20 mg/mL clear
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: 5 mg/mL (requires heating and sonication)
chloroform: 1 mg/mL (requires heating and sonication)
methanol: 1 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: 4 mg/mL (warming to 60 °C for 15 minutes)
H2O: <2 mg/mL
SML0623   Iniparib ≥98% (HPLC) 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: 5 mg/mL clear
SML1843 Kurarinone ≥98% (HPLC) Kurarinone, a flavanone from Sophora flavescens roots, is a potent activator of the large-conductance calcium-activated potassium channel (BKCa channel). Kurarinone exhibits strong preference to potentiate the homomeric BKCa channel composed only of the α subunits. Kurarinone reduces acetylcholine induced contraction of rat urinary bladder strips and decreased the voiding frequency in a rat OAB model. Kurarinone exhibits cytotoxic and antiinflamatory activity. Kurarinone sensitizes TRAIL-induced tumor cell apoptosis via suppression of NF-KB-dependent cFLIP expression.
DMSO: 20 mg/mL clear
SML0991   LLP-3 ≥98% (HPLC) LLP-3 is a cell-permeable Survivin inhibitor. LLP-3 is an inhibitor of Survivin-Ran complex formation that induces apoptosis in tumor slice cultures, including resistant tumors.
DMSO: 10 mg/mL clear
SRP4928   Lipocalin-2 human recombinant, expressed in E. coli, ≥95% (SDS-PAGE), ≥95% (HPLC) LCN2 (lipocalin 2) potentially connects obesity and its related adipose inflammation. LCN2 has also been implicated in a variety of processes including cell differentiation, tumorigenesis, and apoptosis. It is an early marker of acute kidney injury. LCN2 is upregulated in humans with heart failure. It can associate with MMP9 (matrix metalloproteinase-9) and controls its stability. Changes in the expression of LCN2 are associated with many cancers, including breast, colorectal, pancreatic, ovarian, gastric, thyroid, ovarian, bladder and kidney cancers.
 
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
SML1793 MI-4F ≥98% (HPLC) MI-4F is mesoionic compound that exhibits potent anticancer activity against multiple cancer cell lines and in vivo. MI-4F induces apoptosis in HepG2 cells. MI-4F appears to inhibit calcium efflux through inhibition formation of mitochondrial permeability transition pore (MPTP). MI-4F inhibits superoxide dismutase. MI-4F is not susceptible to MDR transporters P-glycoprotein, ABCG2 and MRP1. MI-4F also inhibits ABCG2-mediated efflux of mitoxantrone.
DMSO: 10 mg/mL clear
SML0521 ML 210 ≥98% (HPLC) ML 210 induces non-apoptotic cell death in tumor cells expressing the RAS oncogene.
 
SML0978   ML291 ≥98% (HPLC) ML291 specifically activates the apoptotic arm of the cellular unfolded protein response ( UPR) EC50 = 762 nM) with 105-fold selectivity over activation of the adaptive UPR pathway. ML291 induces apoptosis in wild-type mouse embryonic fibroblasts (MEFs), but not in CHOP KO MEFs.
DMSO: 20 mg/mL clear
SMB00431 Mollugin ≥98% (HPLC) Mollugin displays inhibitory activity in arachidonic acid- and collagen-induced platelet aggregation. Mollugin has been reported to inhibit cancer cell proliferation, and has other biological activities including anti-inflammatory and apoptotic effects.
 
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.
 
SML1660 NA-17 ≥98% (HPLC) NA-17 is a fluorescent naphthalimide that induces accumulation of activated p53 in mitochondria and nuclei of NSCLC cells. NA-17 reorganizes the Bak–Bcl-xl complex, promotes p53 phosphorylation without altering the expression of p53, induces cell cycle arrest at the G1 phase and apoptosis. NA-17 exhibits potent anticancer activities in multiple cancer cell lines showing low toxicity to normal cell lines.
DMSO: 5 mg/mL clear (warmed)
SML1156 NID-1 ≥98% (HPLC) NID-1 (Novel Inducer of Death-1) is a cell permeable and potent inducer of energy-dependent non-apoptotic cell death in mammalian cell lines. NID-1 induced cell death is distinct from macroautophagy, but still reacquires ATG5 and the lysosomal hydrolase cathepsin-L.
DMSO: 25 mg/mL clear
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: 2 mg/mL clear (warmed)
SML1601 NSC59984 ≥98% (HPLC) NSC59984 targets various mutant p53 to restore wild-type p53 pathway via the activation of p73 in cancer cells. NSC59984 depletes a gain of function (GOF p53 mutants. NSC59984 is not cytotoxic against normal cells.
DMSO: 5 mg/mL clear (warmed)
SML1302 Nap-FF ≥98% (HPLC) Nap-FF (2-Naa-FF) is a cell penetrant dipeptide that self-assembly and adopt the β-sheet structures to form prion-like nanofibrils of small molecules (PriSM). PriSM of Nap-FF are selectively cytotoxic to gliomas cancer cells in a presence of stromal cells. PriSM of Nap-FF selectively accumulate in cancer cells, impedes the dynamics of cytoskeletal filaments, and induces apoptosis.
DMSO: 20 mg/mL clear
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.
 
SML1372 Nifetepimine ≥95% (HPLC) Nifetepimine is a dihydropyrimidone calcium channel blocker that down-modulates SERCA3 (sarco/endoplasmic reticulum Ca2+ -ATPase 3) pump, and protects of the CD4+ T cells from tumor-induced apoptosis. Nifetepimine induces apoptotic cell death in triple negative breast cancer (TNBC) cells by stimulation of cross-talk between ER stress and the MEK/ERK pathway.
DMSO: 10 mg/mL clear
SML0610   Nitidine chloride ≥97% (HPLC) 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: 1 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: 20 mg/mL
H2O: insoluble
SML0580 Nutlin-3a ≥98% (HPLC) 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: 5 mg/mL clear
K4394 PKF118-310 ≥98% (HPLC) 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.
H2O: 10 mg/mL clear
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
SML1013 PRT4165 ≥98% (HPLC) PRT4165 is a potent inhibitor of PRC1 (polycomb-repressive complex 1)-mediated histone H2A ubiquitylation in vivo and in vitro. PRT4165 inhibits the in vitro histone H2A E3 ubiquitin ligase activity of PRC1 components RING1, RNF2, and a BMI1/RNF2 complex. PRT4165 also inhibits DNA double-strand breaks induced ubiquitylation of histone H2AX.
DMSO: 20 mg/mL clear
SML1490   Pemetrexed disodium heptahydrate ≥98% (HPLC) Pemetrexed is antifolate cancer drug approved for treatment of variety of cancer including pleural mesothelioma and non-small cell lung cancer. Pemetrexed is a folate antimetabolite that inhibits thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase, three enzymes used in purine and pyrimidine synthesis.
H2O: 30 mg/mL clear
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 clear
P0103   Prodigiosin hydrochloride from Serratia marcescens, ≥98% (HPLC), powder Prodigiosin (PG) exhibits antibacterial, anticancer, cytotoxic, immunosuppressive and antiproliferative activities. Prodigiosin stimulates apoptosis in hematopoietic cancer cells and in cells derived from other human cancers, such as gastric and colon, with no marked toxicity in nonmalignant cell lines. In addition, prodigiosin also has p53-independent anti-proliferative activity. Experimental studies show that prodigiosin promotes various cellular processes such as cell shrinkage, chromatin condensation, restructuring of actin microfilament network and detachment of cells from the cell culture substrate. Different targets and mechanisms of action were described for prodigiosin, including induction of single- and double stranded DNA breaks modulation of pH, regulation of mitogen-activated protein kinase, and inhibition of cell cycle progression.
Prodigiosin, a tripyrrole red pigment biosynthesized by Serratia marcescens and other bacteria, exhibits antibacterial, anticancer, cytotoxic, immunosuppressive, and antiproliferative activities. 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. 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. 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.
DMSO: soluble
H2O: insoluble
acetonitrile: soluble
chloroform: soluble
methanol: soluble
SML0932   Psoralidin ≥98% (HPLC) Psoralidin is a furanocoumarin natural product used in Chinese medicine. Psoralidin, a PTP1B inhibitor, has been shown to have anticancer activity with a variety of mechanisms proposed. Psoralidin induces ROS generation in androgen-independent prostate cancer cells, leading to inhibition of cell proliferation. Psoralidin has been found to downregulate NOTCH1 signaling, causing growth arrest in both breast cancer stem cells and breast cancer cells.
DMSO: 5 mg/mL clear (warmed)
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
SML1745 Raptinal ≥95% (HPLC) Raptinal is a cell-permeable bifluorene-dicarbaldehyde compound that acts as a rapid activator of mitochondrial pathway-mediated intrinsic apoptosis.
DMSO: 5 mg/mL clear (warmed)
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. In a related report 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
SML0892   Roslin 2 ≥98% (HPLC) Roslin 2 is a p53 reactivator that disrupts the FAK and p53 interaction, and reactivates transcriptional activity of p53 with p21, Mdm-2 and Bax transcriptional targets. Roslin 2 decreases viability and clonogenicity of cancer cells, and inhibits tumor growth.
H2O: 20 mg/mL clear
SML1306 S-p-Bromobenzylglutathione cyclopentyl diester ≥98% (HPLC) S-p-Bromobenzylglutathione cyclopentyl diester (BBGC) is a cell-permeable inhibitor of Glyoxalase 1 (GLO1), an enzyme that detoxifies methylglyoxal, a toxic side-product of glycolysis that induces apoptosis at high levels and has been linked to arterial atherogenesis in diabetics. However, tumors use GLO as well and overexpression of GLO1 has been reported in a number of cancers, so GLO1 inhibitors including BBCG have been investigated as possible anticancer agents. Recent studies have indicated that methylglyoxal has some beneficial effects at low levels with GABAA receptor agonist activity, and that GLO1 inhibition with BBGC can reduce anxiety-like behavior and decrease antiseizure activity. S-p-bromobenzylglutathione cyclopentyl diester should be an inportant tool to study the glyoxalase system.
DMSO: 20 mg/mL clear
S7451 SJ-172550 ≥95% (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
SML1464 SMBA1 ≥98% (HPLC) SMBA1 is a potent and selective Bax agonist that binds to Bax, induces conformational change which blocks Bax S184 phosphorylation. SMBA1 induces apoptosis in cancer cells and suppresses lung tumor growth in vivo without significant normal tissue toxicity. SMBA1 does not bind to other Bcl-2 family members.
DMSO: 20 mg/mL clear
S7448 STF-62247 ≥98% (HPLC), solid STF-62247 induces the formation of large vacuoles in the von Hippel-Lindau deficient renal carcinoma cells, a characteristic of autophagy.1
STF-62247 is a selective inducer of autophagy in VHL-deficient renal cell carcinoma cells.
DMSO: soluble 26 mg/mL
H2O: insoluble
SML1493   Suprafenacine ≥98% (HPLC) Suprafenacine is a cell permeable and potent microtubule destabilizing agent that induces cell cycle arrest in the G2/M phase and apoptotic cell death. Suprafenacine binds to microtubules at the colchicine-binding and inhibits polymerization. Suprafenacine is selective for cancer cells including drug-resistant cancer cells. Apparently, Suprafenacine bypasses the multidrug resistance transporter P-glycoprotein (PGP).
DMSO: 10 mg/mL clear
SML1908 Syrosingopine ≥95% (HPLC) Syrosingopine is an antihypertensive agent related to reserpine that was found to potentiate the anticancer effects of the antidiabetic agent metformin and phenformin without harmful effects on normal cells. Syrosingopine was also found to potentiate the anticancer activity of mitochondrial electron transport chain (ETC) inhibitors. Its mechanism of action is currently unknown but may involve inhibition of glycolytic enzyme α-enolase rather than its known activity as an inhibitor of vesicular monoamine transporters VMAT1 and VMAT2.
DMSO: 10 mg/mL clear
SML1710   Talniflumate ≥98% (HPLC) Talniflumate is an orally available, potent and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2 b-1,6 N-acetylglucosaminyltransferase). Talniflumate decreases GCNT3 expression and production of mucins in vivo and in vitro. Talniflumate improves responsiveness of pancreatic tumors to gefitinib. Talniflumate is a potent calcium-activated chloride channel (CaCC) blocker.
DMSO: 5 mg/mL clear (warmed)
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.
Taurolidine is an antibacterial agent that can be used for the treatment of peritonis. It has also been used as an antiendoxic substance for systematic inflammatory response syndrome and as an anti-angiogenic agent for tumors. Furthermore, studies have reported that taurolidine can be used for the prevention of multiple catheter-related bloodstream infections.
DMSO: >20 mg/mL
SML1707   Temoporfin ≥90% (HPLC) Temoporfin is a photosensitizer for the photodynamic therapy. Temoporfin has been used clinically to treat advanced head and neck squamous cell carcinoma, and is being investigated for use in several other cancers.
DMSO: 2 mg/mL clear (warmed)
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: 10 mg/mL clear
H2O: insoluble
SML1758 Tetrazanbigen ≥98% (HPLC) Tetrazanbigen (TNBG) is a potent and selective antitumor drug that induces lipid accumulation in cancer cells. Tetrazanbigen induces S phase arrest and apoptosis in hepatocellular carcinoma QGY-7701. Tetrazanbigen potently inhibits growth of QGY-7701 cells xenografts in mice.
DMSO: 5 mg/mL clear (warmed)
SML1456 Thaxtomin A ≥98% (HPLC) Thaxtomin A is a nitrated diketopiperazine phytotoxin produced by Streptomyces scabies that induces plant cells necrosis. Thaxtomin A is a potent plant cellulose synthesis inhibitor.
 
SML0954   Thiocolchicine ≥97% (HPLC) Thiocolchicine is an antimitotic alkaloid and apoptosis inducer that inhibits tubulin polymerization and microtubule assembly.
DMSO: 10 mg/mL clear
SML0552 Tirapazamine ≥98% (HPLC) 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: 10 mg/mL clear
SML0821 UCD38B hydrochloride ≥98% (HPLC) UCD38B is a cell permeable inhibitor of intracellular uPA (urokinase plasminogen activator) that is cytotoxic to proliferating and non-proliferating glioma cell lines. UCD38B induces caspase-independent necrosis in U87 glioma MDA231 breast cancer cells. It appears that the necrotic pathway is mediated by AIF (apoptotic inducible factor).
DMSO: 15 mg/mL clear
SML1492 UMI-77 ≥98% (HPLC) UMI-77 is an inhibitor of Induced myeloid leukemia cell differentiation protein Mcl-1, a member of the Bcl-2 family that inhibits apoptosis. UMI-77 acts by binding to the BH3-binding groove of Mcl-1, blocking the heterodimerization of Mcl-1/Bax and Mcl-1/Bak. UMI-77 is selective for Mcl-1 over other members of the antiapoptotic Bcl-2 family with a Ki of 490 nM. It inhibited cell growth and induced apoptosis in pancreatic cancer cells.
DMSO: 20 mg/mL clear
SML1576 Undecylprodigiosin hydrochloride ≥95% (HPLC) Undecylprodigiosin is a tri-pyrolle antibiotic isolated from Streptomyces coelicolor A3 that exhibits immunosuppressive and apoptotic activities as well as antibacterial, antioxidative and UV protective properties. Undecylprodigiosin selectively induces p53 independent apoptosis in cancer cells.
 
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: 10 mg/mL (clear solution)
SML1187   Vacquinol-1 dihydrochloride ≥98% (HPLC) Vacquinol-1 (NSC13316) is a brain penetrant inducer of catastrophic vacuolization in glioblastoma cells (GCs). Vacquinol-1 displays high cytotoxicity to GCs; it induces cell death by membrane ruffling, cell rounding, massive macropinocytic vacuole accumulation, ATP depletion, and cytoplasmic membrane rupture of GCs. Vacquinol-1 originally was developed as an antimalarial compound.
DMSO: 5 mg/mL clear (warmed)
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. Violacein exhibits antitumoral, antibacterial, antiulcerogenic, antileishmanial, and antiviral activities. Violacein and its β-cyclodextrin complexes trigger apoptosis and differentiation in HL60 leukemic cells. Violacein cytotoxicity is preceded by activation of caspase 8, transcription of NF-κB target genes, and p38-MAPK activation resembling TNF-α signal transduction.
H2O: insoluble
acetone: soluble
ethanol: soluble
methanol: soluble
SML1823 Vosaroxin hydrochloride ≥98% (HPLC) Vosaroxin is an anti-cancer quinolone derivative that acts as a DNA intercalator and a topoisomerase II inhibitor, causing p53 independent tumor cell apoptosis. Vosaroxin stabilizes cleavage complexes formed by topoisomerase IIα and IIβ, which results in an accumulation of DNA double-strand breaks. Vosaroxin showed antineoplastic activity in multiple solid tumor and hematologic cancer cell lines and has been in clinical trials for AML.
H2O: 1 mg/mL clear (warmed)
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.