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Apoptosis Inhibitors



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10058-F4 ≥98% (HPLC), solid 10058-F4 is a c-Myc inhibitor that induces cell-cycle arrest and apoptosis. It 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 mM using c-Myc transfected Rat1a fibroblasts).
DMSO: >10 mg/mL
H2O: <2 mg/mL
F3680pricing
 BAX Inhibiting Peptide V5 ≥97% (HPLC), lyophilized powder Bax-mediated apoptosis inhibitor; membrane permeable pentapeptide based on the Ku70-Bax inhibiting domain.
B1436pricing
BBMP ≥98% (HPLC), solid BBMP is a mitochondrial permeability transition pore (PTP) inhibitor. PTP inhibitors and mitochondrial depolarization are potential therapeutics for neurodegenerative diseases.
DMSO: 16 mg/mL
H2O: <2 mg/mL
B7936pricing
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
B2938pricing
BI-6C9 ≥97% (HPLC), solid BI-6C9 is a tBid inhibitor and antiapoptotic.
DMSO: 24 mg/mL
H2O:  insoluble
B0186pricing
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.
B6179pricing
Clofarabine ≥98% (HPLC), solid Clofarabine is toxic to nondividing lymphocytes and monocytes. It is a better substrate for deoxycitidibe kinase then CdA.
DMSO: >10 mg/mL
H2O: >12 mg/mL
C7495pricing
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
C7744pricing
Cyclic Pifithrin-α >95% (HPLC) A stable analog of Pifithrin-α (Product Code P4359) with similar biological activities and lower cellular toxicity.
DMSO: 20 mg/mL
P4236pricing
Fasentin ≥98% (HPLC) New Fastenin is a novel of glucose uptake, GluT1 inhibitor. Evasion of death receptor ligand-induced apoptosis is an important contributor to cancer development and progression. Therefore, molecules that restore sensitivity to death receptor stimuli would be important tools to better understand this biological pathway and potential leads for therapeutic adjuncts. Fasentin is a novel inhibitor of glucose uptake that sensitizes cells to FAS-induced cell death. Fasentin was screened out from 2000 compounds. Fasentin selectively sensitized to death ligands, but did not decrease FLIP expression. Fasentin 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. It highlights a new mechanism to sensitize cells to death ligands. Dipyridamole (Cat. No. D9766), which is a weak GluT inhibitor which partially inhibits glucose uptake ane sensitize cells to FAS. Two glucose uptake inhibitor, phloretin (Cat. No. P3449) & cytochalasin B (Cat. No. C6762), have been reported to be highly toxic and not sensitize cells to FAS.
DMSO: >10 mg/mL
F5557pricing
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
G9420pricing
MDL 28170 ≥95% (HPLC) 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
M6690pricing
Mdivi-1 ≥98% (HPLC) New Mdivi-1 is a selective inhibitor of mitochondrial division DRP (dynamin-related GTPase); 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
M0199pricing
N-Ethylmaleimide SigmaUltra, ≥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 colorless to faint yellow, clear to slightly hazy
E1271pricing
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.
E3876pricing
NS3694 ≥98%, solid Inhibitor of apoptosome formation.
DMSO: 22 mg/mL, soluble
H2O: <5 mg/mL, insoluble
N7787pricing
NSCI ≥97% (HPLC), solid NSCI is a nonpeptide caspase 3 selective inhibitor.
DMSO: >10 mg/mL
H2O:  insoluble
N1413pricing
Necrostatin-1 ≥98% (HPLC), solid Necrostatin-1 is an inhibitor of necroptosis (non-apoptotic cell death pathway).
DMSO: >10 mg/mL
N9037pricing
 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
O9639pricing
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
P4359pricing
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: >10 mg/mL
H2O: <2 mg/mL
P0122pricing
R5C3 ≥97% (HPLC), solid MDM2 inhibitor, 2-phenoxybenzoyl-tryptophan derivative. Reported as a novel probe for high throughput fluorescence polarization binding assay. Useful in drug screening for small molecule inhibitors of MDM2-binding to p53.
DMSO: 18 mg/mL
R7529pricing
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.
DMSO: 16 mg/mL, soluble
H2O:  insoluble
S5944pricing