1. Signaling Pathways
  2. Apoptosis
  3. Necroptosis

Necroptosis (坏死性凋亡)

Necroptosis is a form of regulated necrotic cell death mediated by receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like (MLKL) and generally manifests with morphological features of necrosis. Necroptosis is characterized by early loss of plasma membrane integrity, leakage of intracellular contents, and organelle swelling. The cells dying through necroptosis lack the typical apoptotic characteristics, such as membrane blebbing, chromatin condensation, and intranucleosomal DNA cleavage into 180 bp DNA laddering, but may show TUNEL positivity.

Necroptosis triggers innate immune responses by rupturing dead cells and releasing intracellular components, it can be caused by Toll-like receptor (TLR)-3 and TLR-4 agonists, tumor necrosis factor (TNF), certain microbial infections, and T cell receptors. Necroptosis signaling is modulated by receptor-interacting protein kinase (RIPK) 1 when the activity of caspase-8 becomes compromised. Activated death receptors (DRs) cause the activation of receptor-interacting serine-threonine kinase 1 (RIPK1) and the RIPK1 kinase activity-dependent formation of an RIPK1-RIPK3-MLKL, which is complex II. RIPK3 phosphorylates MLKL, ultimately leading to necrosis through plasma membrane disruption and cell lysis.

Necroptosis 相关产品 (11):

目录号 产品名 作用方式 纯度
  • HY-134050
    Apostatin-1 Inhibitor 99.24%
    Apostatin-1 (Apt-1) 是一种有效的 TRADD 抑制剂。Apostatin-1 可与 TRADD-N 结合 (KD=2.17 μM),破坏其与 TRADD-C 和 TRAF2 的结合。Apostatin-1 调节 RIPK1beclin 1 的泛素化。Apostatin-1 通过激活突变 tau、α-synuclein 或 huntingtin 积累的细胞中的自噬 (autophagy),阻断凋亡 (apoptosis),并恢复细胞内稳态。
  • HY-N3417
    Kongensin A Inhibitor ≥98.0%
    Kongensin A 是一种从 Croton kongensis 中分离的天然产物。 Kongensin A 是一种有效的,共价的 HSP90 抑制剂,可阻断 RIP3 依赖性坏死病。Kongensin A 是一种有效的坏死性抑制剂和凋亡诱导剂,并具有潜在的抗坏死性和消炎性应用。
  • HY-135826
    Necroptosis-IN-1 Inhibitor 98.39%
    Necroptosis-IN-1 是 Necrostatin-1 的类似物,是坏死性凋亡的抑制剂,是 RIPK 的抑制剂。
  • HY-144828
    RIP1/RIP3/MLKL activator 1 Inducer
    RIP1/RIP3/MLKL activator 1 (Compound 6i) 是一种有效的抗胶质瘤 (anti-glioma) 药物。RIP1/RIP3/MLKL activator 1 通过激活 RIP1/RIP3/MLKL 通路诱导细胞坏死 (necroptosis)。 RIP1/RIP3/MLKL activator 1 可透过血脑屏障。
  • HY-148382
    RI-962 是一种有效的选择性受体相互作用蛋白激酶 1 (RIPK1) 抑制剂。RI-962 抑制 RIPK1,IC50 值为 35.0 nM。RI-962 可用于神经系统疾病和炎症性疾病的研究。
  • HY-148454
    Necroptosis-IN-3 Inhibitor
    Necroptosis-IN-3 (Compound 69) 是一种坏死性凋亡 (necroptosis) 抑制剂,抑制 TNF-α 诱导的坏死性凋亡。Necroptosis-IN-3 (Compound STX1638) 也抑制 11β-HSD1
  • HY-144277
    RIPK1-IN-12 Inhibitor
    RIPK1-IN-12 是一种有效的 RIPK1 抑制剂,RIPK1-IN-12 能抑制人和小鼠细胞的坏死性凋亡,EC50 值分别为 1.6 和 2.9 nM.
  • HY-117200
    Necrostatin-7 Inhibitor
    Necrotatin-7 (Nec-7) 是一种有效的坏死性凋亡 (necroptosis) 抑制剂,EC50 为 10.6 μM。 Necrotatin-7 不抑制重组 RIP1 激酶。
  • HY-151541
    MLKL-IN-3 Inhibitor
    MLKL-IN-3 (compound 66) 是一种有效的 MLKL (混合谱系激酶结构域样蛋白)抑制剂。MLKL-IN-3 可抑制 HT-29 细胞的坏死 (necroptosis),作用于 MLKL 磷酸化的下游,其 EC50 为 31 nM。
  • HY-N10520
    Pectic acid Inducer
    Pectic acid (Methyl protopectin) 是一种聚半乳糖醛酸,可诱导垂体肿瘤细胞凋亡 (apoptosis) 和坏死 (necrosis)。Pectic acid 可用于癌症和自身免疫性疾病的研究。
  • HY-151542
    MLKL-IN-4 Inhibitor
    MLKL-IN-4 (compound 56) 是一种有效的 MLKL (混合谱系激酶结构域样蛋白)抑制剂。MLKL-IN-4 可抑制 HT-29 细胞的坏死 (necroptosis),作用于 MLKL 磷酸化的下游,其 EC50 为 82 nM。