necroptosis

Necroptosis-IN-1 is a potent necroptosis inhibitor of RIPK1. It is an analog of Necrostatin-1.

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.

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.

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.

CDDO-3P-Im is an orally active inhibitor of necroptosis with chemopreventive effects. CDDO-3P-Im can be used in studies about ischemia/reperfusion.

Apostatin-1 (Apt-1) is a novel TRADD inhibitor that binds to a pocket on the N-terminal TRAF2 binding domain of TRADD.

Necroptosis-IN-5 (Compound 26) is an orally active inhibitor of necroptotic cell death (necroptosis). This compound also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). It can be utilized in research related to inflammatory diseases, neurodegenerative disorders, and cancer associated with necroptosis.

Necroptosis-IN-4 is an effective inhibitor of necroptosis, specifically targeting RIP kinase 1 (RIPK1) without inhibitory activity against RIPK3. It exhibits weak inhibitory effects on VEGFR1 2 and PDGFR-α.

Necrostatin 2 racemate (Necrostatin-2 racemate) is an potent and specific inhibitor of RIPK1.

Necrostatin-34 (2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4) is a RIPK1 kinase inhibitor, stabilizing RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.

ZZW-115 hydrochloride inhibits the activity of NUPR1.

Glyphosate (Atila) is an herbicide. It also is a possible carcinogen to humans.

Necrostatin-7 (Necrostatin 7) is an inhibitor of necrotic apoptosis with cardioprotective effects, inhibits RANK-NFATc1 signaling, and attenuates macrophage differentiation into osteoblasts.

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.

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.

TopoisomeraseI II inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of TopoisomeraseI II that induces DNA damage and activates PARP-1, leading to the activation of RIPK1, RIPK3, and MLKL, ultimately causing necroptosis. It shows significant anticancer activity by effectively targeting cancer cell nuclei and inducing cell death through necroptosis, offering substantial clinical potential in overcoming resistance in cancer treatment.

Anticanceragent 267 (Compound 5q) serves as an activator of RIPK3 and MLKL. It effectively inhibits the proliferation of several cancer cell lines, with IC50 values of 9.79, 10.77, and 5.94 μM for MDA-MB-231, MDA-MB-486, and MCF-7, respectively. The compound induces cell cycle arrest at the subG1 phase and triggers necroptosis in MDA-MB-231 cells. Additionally, Anticanceragent 267 demonstrates antitumor activity in mouse xenograft models.

ZYH-23 is a potent inhibitor of necroptosis. It targets HSP90 to inhibit the phosphorylation of RIPK1, RIPK3, and MLKL, effectively blocking programmed cell necrosis.

RIPK1-IN-20 has strong RIPK1 kinase inhibitory activity with an IC50 value of 59.8 nM. It can block TNFα-induced necroptosis in both human and mouse cells, with an EC50 ranging from 1.06 to 4.58 nM.

Kongensin A is an effective heat shock protein 90 (HSP90) inhibitor that has potential anti-necroptosis and anti-inflammation applications.

RIPK1-IN-12 is a potent inhibitor of RIPK1, exhibiting an inhibitory effect on necroptosis in human and mouse cells with EC50 values of 1.6 and 2.9 nM, respectively.

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.

SZM-1209 is a potent and specific RIPK1 inhibitor with oral activity, displaying a dissociation constant (Kd) of 85 nM. It demonstrates substantial anti-necroptotic efficacy with an EC50 of 22.4 ± 8.1 nM and possesses therapeutic effects against systemic inflammatory response syndrome (SIRS) and acute lung injury (ALI) [1].

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].