Apoptosis Inhibitors

Sigma offers several small molecules that inhibit a cell’s initiation of or progression through the apoptosis process. This set of compounds includes inhibitors of c-Myc, Bax, p53, tBid, and BCL that mediate apoptosis as well as caspase inhibitors and other enzymes involved in the apoptotic pathways. Apoptosis inhibitors are important research tools when investigating the cellular mechanisms underlying stroke, spinal cord injuries, multiple sclerosis, artherosclerosis, and cancer.

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F3680 10058-F4 ≥98% (HPLC), solid 10058-F4 is a c-Myc inhibitor that induces cell-cycle arrest and apoptosis. 10058-F4 is a cell-permeable thiazolidinone that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 inhibits tumor cell growth in a c-Myc-dependent manner both in vitro and in vivo (64 μM using c-Myc transfected Rat1a fibroblasts).
DMSO: >10 mg/mL
H2O: <2 mg/mL
SML0699   4′-Methoxyflavone ≥97% (HPLC) 4-methoxyflavone is a neuroprotective agent that inhibits the accumulation of poly (ADP-ribose) and neuronal cell death following chemically-induced DNA damage or NMDA excitation.
DMSO: 5 mg/mL clear (warmed)
SML1855   AZD5438 ≥97% (HPLC) AZD5438 is an orally active, potent and reversible inhibitor against cyclin-dependent kinases (IC50 = 6 nM/Cyc E-CDK2, 14 nM/p25-CDK5, 16 nM/Cyc B1-CDK1, 20 nM/Cyc T-CDK9, 21 nM/Cyc D3-CDK6, 45 nM/Cyc A-CDK2, 449 nM/Cyc D1-CDK4, 821 nM/Cyc H-CDK7; [ATP] = Km) and glycogen synthase kinase GSK-3β≤ (IC50 = 17 nM) without significant inhibitory potency toward 30 other kinases (≤75% inhibition at 10 μM). AZD5438 effectively inhibits cellular CDK substrates phosphorylation and displays antiproliferation activity against a broad spectrum of human cancer cultures (IC50 from 0.2 μM/MCF to 1.7 μM/ARH-77) by inducing cell cycle arrest at G2-M, S, and G1. Oral administration (50 mg/kg/12 h or 75 mg/kg/day) is efficacious against human tumor xenograft growth in mice in vivo.
DMSO: 20 mg/mL clear
SRP5165 BAG1 (72-end), GST tagged human recombinant, expressed in E. coli, ≥70% (SDS-PAGE), buffered aqueous glycerol solution    
B1436   BAX Inhibiting Peptide V5 ≥97% (HPLC), lyophilized powder Bax-mediated apoptosis inhibitor; membrane permeable pentapeptide based on the Ku70-Bax inhibiting domain.
 
B2938 BEPP monohydrochloride ≥98% (HPLC) BEPP is a double-strand RNA-dependent protein kinase (PKR) activator. The double-strand RNA (dsRNA)-dependent protein kinase is a ubiquitously expressed serine threonine kinase, inducible by interferon γ. PRK is involved in several curtail cellular regulations including phosphorylation of eIF2α (which leads to inhibition of protein synthesis and eliciting antivirus and antitumor activities), modulating activities of eIF2α, NF-κB, ATF-3, and p53. BEPP also inhibits the growth of a human lung cancer cell line overexpressing PKR.
DMSO: >10 mg/mL
B0186 BI-6C9 ≥97% (HPLC), solid BI-6C9 is a tBid inhibitor and antiapoptotic.
DMSO: >20 mg/mL
SML0121 BTZO-1 ≥98% (HPLC) BTZO-1 is a suppressor of cardiomyocyte apoptosis presumably by activation of antioxidant response element (ARE)-mediated gene expression. BTZO-1 binds to the macrophage migration inhibitory factor (MIF) that is required to activate the glutathione S-transferase Ya subunit (GST Ya) gene ARE.
DMSO: ≥7 mg/mL
B6179 Bongkrekic acid solution from Pseudomonas cocovenenans, ≥95% (HPLC), ~1 mg/mL An antiapoptotic agent, it protects against NMDA receptor induced neuronal apoptosis,­ extends cell survival in cells undergoing apoptosis following infection with viral vectors and abrogates apoptosis induced by hydrogen peroxide in T-cells. It is an inhibitor of adenine nucleotide translocase, which is a component of the mitochondrial permeability transition (MPT) pore complex. Bongkrekic acid prevents mitochondrial depolarization, swelling, rupture of mitochondrial outer membrane, and release of apoptogenic proteins such as cytochrome c. This phenomenon was observed during staurosporine induced apoptosis in Jurkat cells, in HepG2 undergoing apoptosis following TNF-α and ethanol.
 
SML0068 CTP Inhibitor ≥98% (HPLC) CTP Inhibitor is an inhibitor of mitochondrial citrate transport protein, was the first purely competitive inhibitor to be discovered and is more potent than BTC.
CTP inhibitor blocks the exchange of tricarboxylates the key intermediates in anabolism and catabolism by mitochondrial citrate transport protein (CTP).
DMSO: ≥23 mg/mL
SML1754   CTX1 ≥95% (HPLC) CTX1 is a potent HdmX inhibitor that overcomes HdmX-mediated p53 repression. CTX1 inhibits proliferation and induces apoptosis in number of cancer cell lines. CTX1 inhibits growth of primary human AML in immunodeficient mice.
DMSO: 15 mg/mL clear
C8999 Calpeptin ≥98% (HPLC) Calpeptin is a rho kinase activator and an inhibitor of calpains, a family of calcium-dependent cysteine proteases involved in apoptosis, long-term potentiation in neurons, and cell cycle progression.
DMSO: 15 mg/mL clear
C7495 Clofarabine ≥98% (HPLC) Clofarabine is a purine nucleoside antimetabolite. Clofarabine is toxic to nondividing lymphocytes and monocytes.
DMSO: >10 mg/mL
SRP8003   Clusterin (nuclear form) mouse recombinant, expressed in E. coli, His tagged, >90% (SDS-PAGE) Clusterin is involved in tissue remodeling, cell death, lipid transport, complement-associated cell lysis, cancer and neurological damage. It is strongly expressed in Alzheimer’s and treatment-resistant cancer. High levels of clusterin are observed in ischemic heart disease and diabetic conditions. It also protects kidney from fibrosis. Nuclear form of clusterin works as a pro-death signal, and suppresses cell growth and survival. The secreted form of clusterin has extracellular chaperone and anti-apoptotic activities.
 
SRP8004   Clusterin (secretory form) human recombinant, expressed in HEK 293 cells, FLAG® tagged, >90% (SDS-PAGE)    
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
P4236 Cyclic Pifithrin-α hydrobromide ≥98% (HPLC) A stable analog of Pifithrin-α (Product Code P4359) with similar biological activities and lower cellular toxicity.
DMSO: 20 mg/mL
SML0183 EM20-25 ≥98% (HPLC) EM20-25 disrupts the BCL-2/BAX interactions and activates caspase-9 in cells overexpressing BCL-2. It sensitizes the BCL-2 expressing leukemic cells to the effects of chemotherapy involving staurosporine and chlorambucil.
EM20-25 is an analog of HA14-1 that antagonizes the effects of the anti-apoptotic protein BCL-2, and causes opening of the mitochondrial permeability transition pore. Unlike HA14-1, EM20-25 does not effect mitochondrial respiration.
DMSO: ≥5 mg/mL at ~60 °C
F5557 Fasentin ≥98% (HPLC) Fasentin is a novel inhibitor of glucose uptake, GluT1 inhibitor. Fasentin is a novel inhibitor of glucose uptake that sensitizes cells to FAS-induced cell death. Fasentin selectively sensitized to death ligands, but did not decrease FLIP expression. It alters expression of genes associated with nutrient and glucose deprivation. Fasentin interacted with a unique site in the intracellular channel of the glucose transport protein GLUT1.
DMSO: >10 mg/mL
SML0583   Ferrostatin-1 ≥95% (HPLC) Ferrostatin-1 is a potent inhibitor of non-apoptotic cell death induced by erastin call ferroptosis. Ferrostatin-1 prevents ferroptopic cell death in cancer cells and glutamate-induced toxicity in organotypic rat brain slices. It appears that Ferrostatin-1 controls lipid soluble ROS.
DMSO: 10 mg/mL clear
G9420 GNF-2 ≥98% (HPLC), solid GNF-2 belongs to a new class of Bcr-abl inhibitors. GNF-2 appears to bind to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. It inhibits Bcr-abl phosphorylation with an IC50 of 267 nM, but does not inhibit a panel of 63 other kinases, including native c-Abl, and shows complete lack of toxicity towards cells not expressing Bcr-Abl. GNF-2 shows great potential for a new class of inhibitor to study Bcr-abl activity and to treat resistant Chronic myelogenous leukemia (CML), which is caused the Bcr-Abl oncoprotein.
DMSO: ≥5 mg/mL
H2O: <2 mg/mL
SML0412 IM-54 ≥98% (HPLC) IM-54 is a cell permeable, potent and selective inhibitor of necrosis. The compound inhibits necrosis induced by oxidative stress. IM-54 does not inhibit apoptosis induced by anticancer drugs.
DMSO: 5 mg/mL (clear solution)
410960 Ischemin - Calbiochem A cell-permeable azobenzene compound that reversibly targets CBP-BRD acetyl-lysine binding pocket with moderate selectivity over BAZ1B, PCAF, BRD4-1 and BAZ2B.    
SML1414 Liproxstatin-1 >98% (HPLC) Liproxstatin-1 is a potent inhibitor of ferroptosis, a non-apoptotic form of cell death characterized by iron-dependent accumulation of lethal lipid reactive oxygen species (ROS). Liproxstatin-1 suppressed ferroptosis in human cells and in an ischaemia/reperfusion-induced tissue injury model in mice. Knockout of glutathione peroxidase 4 (Gpx4) Has been shown to cause cell death by ferroptosis. Liproxstatin-1 was able to suppress ferroptosis in Gpx4 knock-out mice.
DMSO: 10 mg/mL clear
M6690 MDL 28170 ≥95% (HPLC) MDL 28170 is a potent cell permeable calpain I and II inhibitor; reduces capsaicin-mediated cell death in cultured dorsal root ganglion neurons. Reduced occurrence of apoptosis in H2O2 and A23187 treated PC12 cells. γ-secretase-inhibitor.
DMSO: 26 mg/mL
H2O: insoluble
methanol: soluble
M0199 Mdivi-1 ≥98% (HPLC), powder Mdivi-1 is a cell-permeable selective inhibitor of mitochondrial division DRP (dynamin-related GTPase) and inhibitor of the mitochondrial division dynamin (Dnm1). Mitochondrial fusion and division play important roles in the regulation of apoptosis. Mdivi-1 is the first selective inhibitor of mitochondrial division dynamins. In principle, Mdivi-1 represents a class of therapeutics for stroke, myocardial infarction, and neurodegenerative diseases.
DMSO: >20 mg/mL
SML0629   Mitochondrial Fusion Promoter M1 ≥95% (HPLC) Mitochondrial Fusion Promoter M1 is a cell permeable hydrazone that enhances mitochondrial fusion. M1 protects cells from mitochondrial fragmentation associated cell death. Mitochondrial Fusion Promoter M1 does not interfere with endoplasmic reticula (ER) and lysosomes morphology.
DMSO: 10 mg/mL clear
E1271 N-Ethylmaleimide BioXtra, ≥98% (HPLC) Augments currents from native M-channels in sympathetic neurons and acts as an opener for KCNQ2, KCNQ4 and KCNQ5 channels.
Sulfhydryl alkylating agent that inactivates NADP-dependent isocitrate dehydrogenase and many endonucleases.
95% ethanol: 50 mg/mL clear to slightly hazy (colorless to faint yellow)
E3876 N-Ethylmaleimide crystalline, ≥98% (HPLC) Augments currents from native M-channels in sympathetic neurons and acts as an opener for KCNQ2, KCNQ4 and KCNQ5 channels.
Sulfhydryl alkylating agent that inactivates NADP-dependent isocitrate dehydrogenase and many endonucleases.
ethanol: 50 mg/mL clear to slightly hazy, colorless to faint yellow or tan
N7787 NS3694 ≥98%, powder NS3694 is an Inhibitor of apoptosome formation.
DMSO: soluble 22 mg/mL
H2O: insoluble <5 mg/mL
N1413 NSCI ≥97% (HPLC), solid NSCI is a nonpeptide caspase 3 selective inhibitor.
DMSO: >10 mg/mL
H2O: insoluble
N9037 Necrostatin-1 ≥98% (HPLC) Necrostatin-1 is an inhibitor of necroptosis (non-apoptotic cell death pathway).
DMSO: >10 mg/mL
O9639   Oridonin ≥98% (HPLC), solid Oridonin has potent anti-tumor activity. Oridonin targets AE (AML1-ETO) oncoprotein. Exposure to oridonin induces apoptosis in AE-bearing leukemic cells through the activation of intrinsic apoptotic pathway and triggering a caspase-3-mediated degradation of AE at D188. The compound also prolonged the lifespan of C57 mice bearing truncated AE-expressing leukemic cells without side effects like suppression of bone marrow or reduction of body weight of animals, and exerted synergic effects while combined with cytosine arabinoside. Additionally, oridonin inhibited tumor growth in nude mice inoculated with t(8;21)-harboring Kasumi-1 cells.
DMSO: >20 mg/mL
H2O: insoluble
SML0402 PD 151746 ≥98% (HPLC) PD 151746 is a potent inhibitor of calpains 1 and 2.
DMSO: 15 mg/mL (clear orange solution)
SML0021 PDI inhibitor 16F16 ≥98% (HPLC) 16F16 is a protein disulfide isomerase (PDI) inhibitor, first identified in a screen for compounds that prevent apoptosis induced by mutant huntingtin protein. 16F16 not only suppressed apoptosis induced by the misfolded protein mutant hungtingtin, it also protected rat neurons from cell death triggered by Aβ peptide. The actions of this inhibitor helped to identify a new mechanism in which a cell death pathway is regulated by protein misfolding via PDI upregulation.
DMSO: 12 mg/mL clear
SML0508 Pentostatin ≥95% (HPLC) Pentostatin is a ring-expanded nucleoside (REN) that potently inhibits adenosine deaminase, which leads to lymphocyte toxicity. Pentostatin is used as anticancer agent to treat leukemia (hairy cell leukemia and chronic lymphocytic leukemia) and is investigated as an agent to treat graft-versus-host disease (GVHD).
H2O: 10 mg/mL clear
P4359 Pifithrin-α ≥95% (HPLC), powder Pifithrin-α is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. Pifithrin-α enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin, etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. Pifithrin-α protects mice from lethal whole body γ-irradiation without an increase in cancer incidence. The protective effect is not seen in p53-null mice or cells expressing a dominant negative mutant of the p53 gene. Protection is conferred by the transient expression of p53 in p53-deficient cell lines.
DMSO: 20 mg/mL
P0122 Pifithrin-μ ≥97% (HPLC), solid Pifithrin-μ is an inhibitor of p53 binding and anti-apoptotic, which directly inhibits p53 binding to mitochondria as well as to Bcl-xL and Bcl-2 proteins. PFTμ rescues cells from lethal γ-irradiation-induced cell death. Because pifithrin-μ shuts down only the p53-mitochondrial pathway without affecting the transcriptional functions of p53, it is superior to pifithrin-α.
DMSO: soluble >10 mg/mL clear
H2O: insoluble
506154 Pifithrin-α, p-Nitro, Cyclic - CAS 60477-38-5 - Calbiochem A cell-permeable p53 inhibitor that exhibits 10-fold higher potency and 50% longer half-life than Pifithrin-α.    
506155 Pifithrin-μ - CAS 64984-31-2 - Calbiochem Pifithrin-μ, CAS 64984-31-2, is a cell-permeable inhibitor of p53 interaction with Bcl-xL & Bcl-2. Inhibits p53 translocation to mitochondria without affecting the transactivation function of p53., A cell-permeable sulfonamide that blocks p53 interaction with Bcl-xL and Bcl-2 proteins and selectively inhibits p53 translocation to mitochondria without affecting the transactivation function of p53.    
SML0221 Piperlongumine ≥97% (HPLC) Piperlongumine selectively kills cancer cells regardless of p53 status without harming normal cells. It binds to and inihbits proteins known to regulate oxidative stress, in particular, Glutathione S-transferase pi 1 (GSTP1). It increases the level of reactive oxygen species (ROS) and apoptotic cell death in cancer cells with little effect on either rapidly or slowly dividing primary normal cells. Piperlongumine showed significant antitumour effects in a variety of mouse tumour models and inhibited growth of spontaneously formed malignant breast tumours and their associated metastases.
DMSO: ≥5 mg/mL at  warmed to 60 °C
SML0108 R18 trifluoroacetate ≥98% (HPLC) R18 is a competitive inhibitor of the 14-3-3 scaffolding proteins. It binds to the general binding groove of 14-3-3. R18 blocks 14-3-3 interaction with most or all of its client proteins.
 
S5944 S-15176 difumarate salt ≥98% (HPLC), solid Antioxidant and anti-ischemic agent. Also inhibits mitochondrial permeability transition, prevents the early step in apoptosis by preventing collapse of the electrochemical gradient across the mitochondrial membrane. IC50 for in vitro lipid peroxidation is 0.3 μM. IC50 for carnitine palmitoyltransferase (CPT-1) in heart homogenate is 16.8 μM. The shift from fatty acid to glucose oxidation may contribute to anti-ischemic effect.
S-15176 suppresses the mitochondrial permeability transition in response to calcium ions and inorganic phosphate and inhibits the release of cytochrome c in response to silver ions. It exhibits weak protonophoric activity.5
DMSO: soluble 16 mg/mL
H2O: insoluble
SML1105 UCF-101 ≥98% (HPLC) UCF-101 is a selective inhibitor of the pro-apoptotic mitochondrial serine protease Omi/HtrA2, involved in the cellular response to thermal and oxidative stress. Like SMAC/Diablo, Omi/HtrA2 is an inhibitor of IAPs (inhibitor of apoptosis proteins), inhibiting the apoptosis inhibitors, thus resulting in pro-apoptotic activity. In septic rat studies, UCF-101 was found to inhibit apoptosis and have neuroprotective effects on cerebral oxidative injury and cognitive impairment. In aging rats with induced myocardial ischemia/reperfusion (MI/R) injury, UCF-101 treatment decreased XIAP degradation and caspase-3 activity and exerted cardioprotective effects.
DMSO: 5 mg/mL clear (warmed)
506170 p53-Snail binding Inhibitor, GN25 - Calbiochem The p53-Snail binding Inhibitor, GN25 controls the biological activity of p53-Snail. This small molecule/inhibitor is primarily used for Neuroscience applications.