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ApoptosisNecroptosis
Necroptosis is a programmed form of necrosis, or inflammatory cell death. Conventionally, necrosis is associated with unprogrammed cell death resulting from cellular damage or infiltration by pathogens, in contrast to orderly, programmed cell death via apoptosis. The signaling pathway responsible for carrying out necroptosis is generally understood. TNFα leads to stimulation of its receptor TNFR1. TNFR1 binding protein TNFR-associated death protein TRADD and TNF receptor-associated factor 2 TRAF2 signals to RIPK1 which recruits RIPK3 forming the necrosome also named ripoptosome. Phosphorylation of MLKL by the ripoptosome drives oligomerization of MLKL, allowing MLKL to insert into and permeabilize plasma membranes and organelles. Integration of MLKL leads to the inflammatory phenotype and release of damage-associated molecular patterns (DAMPs), which elicit immune responses.
Necroptosis-IN-1
T93051391980-92-9In house
Necroptosis-IN-1 is a potent necroptosis inhibitor of RIPK1. It is an analog of Necrostatin-1.
- $58
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Glyphosate
T198571071-83-6
Glyphosate (Atila) is an herbicide. It also is a possible carcinogen to humans.
- $39
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Apostatin-1
T90792559703-06-7
Apostatin-1 (Apt-1) is a novel TRADD inhibitor that binds to a pocket on the N-terminal TRAF2 binding domain of TRADD.
- $31
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Bardoxolone
Cited
T2915218600-44-3
Bardoxolone (CDDO) is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM. By suppressing reactive oxygen and nitrogen species (ROS RNS) formation, it promotes the cellular control of ROS RNS levels that would lead to DNA damage associated with tumorigenesis. In various Y cell lines, Bardoxolone has been shown to specifically inhibit proliferation and induce apoptosis. Mechanism studies revealed that Bardoxolone is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.
- $68
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CitedCholesteryl Hemisuccinate
T675091510-21-0
Cholesteryl Hemisuccinate (Cholesterol hydrogen succinate) is a highly soluble cholesterol analogue often used in polar solutions for its hepatoprotective, anticancer and tumour growth inhibiting properties. Cholesteryl Hemisuccinate inhibits the hepatotoxicity of acetaminophen and prevents AAP-induced apoptosis and necrosis in hepatocytes. Cholesteryl Hemisuccinate inhibits DNA polymerase and DNA topoisomerase, thereby inhibiting DNA replication and repair as well as cell division.
- $30
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Sulfaphenazole
T4567526-08-9
Sulfaphenazole (Plisulfan) is an inhibitor of CYP2C9 (Ki: 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki: 63/29 μM for CYP2C8/CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19). At 10 μM, sulfaphenazole has been shown to inhibit endothelium-derived hyperpolarizing factor synthase, a CYP450 isozyme in the porcine coronary artery homologous to CYP2C8/9 that generates reactive oxygen species in coronary endothelial cells and modulates vascular tone and homeostasis.
- $50
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CDDO-3P-Im
T136031883650-95-0
CDDO-3P-Im is an orally active inhibitor of necroptosis with chemopreventive effects. CDDO-3P-Im can be used in studies about ischemia/reperfusion.
- $88
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UH15-38
T881012540881-21-6
UH15-38 is a potent and selective RIPK3 inhibitor that blocks necroptosis in alveolar epithelial cells triggered by IAV, useful for studying lung inflammation.
- $123
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Chlorhexidine digluconate
T1495118472-51-0
Chlorhexidine digluconate is a broad-spectrum antiseptic and disinfectant with broad-spectrum antimicrobial activity, inhibits both Gram-positive and Gram-negative bacteria, induces necrosis and apoptosis, and can be used in the study of bacterial infections.
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IM-54
T24160861891-50-1
IM-54 is a cell-permeable, effective, and selective necrosis inhibitor.
- $48
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Necroptosis-IN-3
T64349547698-18-0
Necroptosis-IN-3 (Cyclohexanecarboxamide, N-(2-thienylmethyl)-) (Compound 69) is a Necroptosis inhibitor that inhibits TNF-α induced necroptosis. Necroptosis-IN-3 (Compound STX1638) also inhibits 11β-HSD1.
- $35
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Necrostatin-5
T37558337349-54-9
Necrostatin-5 (Nec-5) is a selective RIP1 kinase inhibitor and cell necrosis inhibitor that prevents the death of Fadd-deficient Jurkat cells treated with TNF-α, with an EC50 of 240 nM.
- $38
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Cholesteryl Hemisuccinate Tris Salt
TF0106102601-49-0
Cholesteryl Hemisuccinate Tris Salt is an acidic cholesteryl ester with hepatoprotective and anticancer activity.Cholesteryl hemisuccinate is a membrane stabilizer in dipalmitoylphosphatidylcholine liposomes containing Chaikosaponin-d, which enhances the anticancer efficacy of cisplatin.Cholesteryl hemisuccinate possesses antitumor activity, inhibits tumor Cholesteryl hemisuccinate has antitumor activity, inhibits tumor growth, inhibits the hepatotoxicity of acetaminophen (AAP) and prevents AAP-induced apoptosis of hepatocytes.Cholesteryl hemisuccinate protects rodents against the toxic effects of acetaminophen, adriamycin, carbon tetrachloride, chloroform, and galactosamine.
- $40
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Necrostatin-7
T25859351062-08-3
Necrostatin-7 (Necrostatin 7) is an inhibitor of necrotic apoptosis with cardioprotective effects, inhibits RANK-NFATc1 signaling, and attenuates macrophage differentiation into osteoblasts.
- $37
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HDL-16
T865652373280-36-3
HDL-16 is a highly effective P2Y14R antagonist with anti-colitis effects, targeting P2Y14R in intestinal epithelial cells to alleviate ulcerative colitis.
- $30
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Cathepsin B
T800529047-22-7
Cathepsin B is a cysteine protease located within the subcellular endosomes and lysosomal compartments that mediates apoptosis and can be used in cancer research.
- $565
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Necrostatin 2
T12203L852391-19-6
Necrostatin 2 is a necrotic protein and receptor-interacting protein kinase 1 (RIPK1) inhibitor used to study inner ear disorders such as sudden deafness, dizziness and tinnitus.
- $57
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Necrocide 1
T780511247028-61-0
Necrocide 1 is a potent inducer of cancer cell necrosis that is not inhibited by caspase blockers, anti-apoptotic BCL2 overexpression, or TNFα neutralization at nanomolar concentrations, and acts through the mitochondrial regulatory pathway.
- $899
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FGFR1/VEGFR2-IN-2
T89865
FGFR1 VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1 VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.
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Anticancer agent 146
T79347
Anticancer Agent 146 (Compound 1.19) acts as a necroptosis inducer and demonstrates anti-tumor efficacy in the MDA-MB-231 mouse xenograft model [1].
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kwcn-41
T748012913223-17-1
KWCN-41, a selective and efficient RIPK1 kinase inhibitor, exhibits an IC50 value of 88 nM. It specifically targets cell necrosis without affecting apoptosis and possesses anti-inflammatory properties [1].
- $116
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Cholicamideβ
T79707
Cholicamideβ (compound 6), a self-assembling small molecule cancer vaccine adjuvant, forms low cytotoxicity virus-like particles and upon binding to peptide antigens, enhances dendritic cell-mediated antigen presentation and induces antigen-specific T-cell responses, with the ability to induce apoptosis and necrosis [1].
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673-A
T71998109437-62-9
673-A is an aldehyde dehydrogenase (ALDH1A) inhibitor that depletes CD133+ cancer stem cells (CSC) in ovarian cancer cell lines. 673-A triggers necroptosis in ovarian CSCs and induces expression of mitochondrial uncoupling proteins (UCP). 673-A also overcomes chemotherapy resistance in vivo.
- $753
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Antitumor agent-145
T857062983120-65-4
Compound Ir5 (Antitumor agent-145) serves as a tumor inhibitor characterized by significant fluorescence and mitochondrial targeting. It promotes anti-cancer activity by inducing necroptosis and stimulating the necroptosis-related immune response [1].
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