1. Signaling Pathways
  2. Apoptosis
  3. Apoptosis

Apoptosis

Apoptosis is a distinctive form of cell death exhibiting specific morphological and biochemical characteristics, including cell membrane blebbing, chromatin condensation, genomic DNA fragmentation, and exposure of specific phagocytosis signaling molecules on the cell surface. Cells undergoing apoptosis differ from those dying through necrosis. Necrotic cells are usually recognized by the immune system as a danger signal and, thus, resulting in inflammation; in contrast, apoptotic death is quiet and orderly.

There are two major pathways of apoptotic cell death induction: The intrinsic pathway, also called the Bcl-2-regulated or mitochondrial pathway, is activated by various developmental cues or cytotoxic insults, such as viral infection, DNA damage and growth-factor deprivation, and is strictly controlled by the BCL-2 family of proteins. The extrinsic or death-receptor pathway is triggered by ligation of death receptors (members of the tumor necrosis factor (TNF) receptor family, such as Fas or TNF receptor-1 (TNFR1)) that contain an intracellular death domain, which can recruit and activate caspase-8 through the adaptor protein Fas-associated death domain (FADD; also known as MORT1) at the cell surface. This recruitment causes subsequent activation of downstream (effector) caspases, such as caspase-3, -6 or -7, without any involvement of the BCL-2 family.

Studies suggest that alterations in cell survival contribute to the pathogenesis of a number of human diseases, including cancer, viral infections, autoimmune diseases, neurodegenerative disorders, and AIDS (acquired immunodeficiency syndrome). Treatments designed to specifically alter the apoptotic threshold may have the potential to change the natural progression of some of these diseases.

Apoptosis 相关产品 (244):

Cat. No. Product Name Effect Purity
  • HY-10227
    Bortezomib Activator 99.97%
    Bortezomib (PS-341) 是一种细胞渗透性、可逆性和选择性的蛋白酶体抑制剂,通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki=0.6 nM)。Bortezomib (PS-341) 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib (PS-341) 是一种抗癌药物,也是第一种用于人类的蛋白酶体抑制剂。
  • HY-13453
    BAY 11-7082 Activator 99.42%
    BAY 11-7082是 NF-κB 抑制剂, 其通过抑制TNF-α诱导的IκB-α磷酸化来降低NF-κB。 BAY 11-7082抑制泛素化蛋白酶 USP7USP21IC50 分别为0.19 μM 和 0.96 μM。
  • HY-13629
    Etoposide Activator 99.65%
    Etoposide (VP-16; VP-16-213) 是用于治疗多种癌症的化疗药物,通过与拓扑异构酶 II 和 DNA 形成复合物来抑制DNA合成。Etoposide 阻断细胞周期 G2 期并诱导细胞凋亡。
  • HY-B1756
    Rotenone Activator 98.12%
    Rotenone 是线粒体电子传递链复合物I抑制剂。 Rotenone 通过促进线粒体活性氧的产生来诱导细胞凋亡。
  • HY-13520
    Nocodazole Activator 98.68%
    Nocodazole是快速可逆的 microtubule 抑制剂。 Nocodazole与β-微管蛋白结合并破坏微管组装/拆卸动力学,从而防止有丝分裂并诱导肿瘤细胞凋亡。Nocodazole 抑制 Bcr-Abl,增强 CRISPR/Cas9 的活性。
  • HY-19696B
    Tauroursodeoxycholate dihydrate Inhibitor
    Tauroursodeoxycholate dihydrate (TUDCA dihydrate; UR 906 dihydrate; Taurolite dihydrate) 是一种内质网应激抑制剂。Tauroursodeoxycholate 显著降低凋亡分子如 caspase-3caspase-12 表达。Tauroursodeoxycholate 也抑制 ERK
  • HY-117282
    JG-98 Activator 99.97%
    JG-98 是一种热休克蛋白 70 (Hsp70) 变构抑制剂,可与 Hsp70 上的保守位点紧密结合,打断 Hsp70-Bag3 相互作用。JG-98 影响癌细胞和肿瘤相关巨噬细胞,显示抗癌活性。
  • HY-N0375
    18α-Glycyrrhetinic acid Activator 99.19%
    18α-Glycyrrhetinic acid,一种饮食衍生的化合物,是 NF-kB 的抑制剂和蛋白酶体 (proteasome) 的激活剂,在多细胞生物中起到促进长寿和抗聚集因子的作用。18α-Glycyrrhetinic acid 诱导细胞凋亡。
  • HY-10971
    Alisertib Activator 99.84%
    Aliertib (MLN 8237) 是一种口服活性和选择性的 Aurora A 激酶抑制剂 (IC50=1.2 nM),与Aurora A 激酶结合,导致有丝分裂纺锤体异常、有丝分裂累积。Aliertib (MLN 8237) 通过靶向白血病细胞中的 AKT/mTOR/AMPK/p38 途径诱导其凋亡和自噬。具有抗肿瘤活性。
  • HY-13251
    Silvestrol Activator 98.00%
    Silvestrol是从Aglaia foveolata的果实和枝条中分离的真核翻译起始因子 (eIF4A) 抑制剂。
  • HY-16046
    Rimiducid Activator 99.81%
    Rimiducid (AP1903) 是二聚化剂,其通过交联 FKBP 结构域起作用,启动 Fas 信号传导,引起凋亡
  • HY-16591
    Birinapant Activator 99.36%
    Birinapant (TL32711) 是一种二价 Smac 模拟物,是 XIAPcIAP1 的强效拮抗剂,Kd 值分别为 45 nM 和小于 1 nM。Birinapant (TL32711) 在体外结合 cIAP1, cIAP2, XIAP 和 ML-IAP 的 BIR3 结构域,诱导完整细胞中 cIAP1 和 cIAP2 的自身泛素化和蛋白酶体降解,从而形成 RIPK1: caspase-8 复合物,caspase-8 活化和诱导肿瘤细胞死亡。Birinapant (TL32711) 优先靶向 TRAF2 相关的 cIAP1 和 cIAP2,随后抑制 TNF 诱导的 NF-κB 活化。
  • HY-10029
    Nutlin (3a) Activator 98.11%
    Nutlin 3a 是 Nutlin-3 的活性异构体,为一种鼠双微体 2 (MDM2) 拮抗剂,抑制 MDM2-p53 相互作用,且稳定 p53 蛋白,因此诱导细胞周期停滞和细胞凋亡。
  • HY-14596
    Genistein Activator 99.68%
    Genistein是一种大豆异黄酮,是一种多重的酪氨酸激酶 (tyrosine kinases,比如 EGFR) 抑制剂,是对多种癌症的化疗剂,主要通过改变细胞凋亡 (apoptosis),细胞周期和血管生成以及抑制转移。
  • HY-19696A
    Tauroursodeoxycholate Sodium Inhibitor
    Tauroursodeoxycholate Sodium 是一种内质网应激抑制剂。Tauroursodeoxycholate 显著降低凋亡分子如 caspase-3caspase-12 表达。Tauroursodeoxycholate 也抑制 ERK
  • HY-B0313
    Hydroxyurea Activator >98.0%
    Hydroxyurea 通过抑制核糖核苷酸还原酶抑制 DNA 合成的细胞凋亡诱导剂。
  • HY-16966
    SBI-0206965 Activator 98.76%
    SBI-0206965 是一种强效, 选择性和细胞渗透性自噬激酶 ULK1 抑制剂, 抑制 ULK1 和 ULK2 激酶活性, IC50 值分别为 108 nM 和 711 nM。
  • HY-19980
    PRIMA-1Met Activator >99.0%
    PRIMA-1Met 是一种突变型 p53 复活剂,可恢复突变型 p53 的野生型构象和功能,并引发肿瘤细胞凋亡。PRIMA-1Met 还抑制硒蛋白硫氧还蛋白还原酶 1 (TrxR1)。
  • HY-19609
    Calicheamicin Activator 98.44%
    Calicheamicin 是一种有效的细胞毒性试剂,可引起DNA双链断裂。
  • HY-100487
    TAK-243 Activator 99.43%
    TAK-243 是一种一流的,选择性的泛素激活酶,UAE (UBA1) 抑制剂 (IC50=1 nM),其阻断了泛素结合,破坏了单泛素信号传导和全蛋白泛素化。TAK-243 诱导内质网应激 (ER) 反应,消除 NF-κB 通路活化,促进细胞凋亡。
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