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APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase that marks target cell cycle proteins for degradation by the 26S proteasome. The APC/C is a large complex of 11–13 subunit proteins, including a cullin (Apc2) and RING (Apc11) subunit much like SCF. The APC/C's main function is to trigger the transition from metaphase to anaphase by tagging specific proteins for degradation. The two proteins of most importance that get degraded in this process as substrates of the APC/C are securin and S and M cyclins. Securin releases separase, a protease, after being degraded which in turn triggers the cleavage of cohesin, the protein complex that binds sister chromatids together. During metaphase, sister chromatids are linked by intact cohesin complexes. When securin undergoes ubiquitination by the APC/C and releases separase, which degrades cohesin, sister chromatids become free to move to opposite poles for anaphase. The APC/C also targets the mitotic cyclins for degradation, resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexes, promoting exit from mitosis and cytokinesis.

  1. Cat.No. 产品名称 Information
  2. GC62419 Apcin-A Apcin-A,是 Apcin 衍生物,是一种后期促进复合物 (APC) 抑制剂。Apcin-A 与 Cdc20 强烈相互作用,抑制 Cdc20 底物的泛素化。Apcin-A 可用于合成 PROTAC CP5V 。
  3. GC18518 Apcin Apcin 是 Cdc20 的配体,是一种有效的竞争性后期促进复合物/环体 (APC/C(Cdc20)) E3 连接酶活性抑制剂。 Apcin 通过与 Cdc20 结合并阻止底物识别竞争性地抑制 APC/C 依赖性泛素化。 Apcin 占据 WD40 结构域侧面的 D-box 结合口袋,可以延长有丝分裂。
  4. GC11469 TASIN-1 TASIN-1 是截短型 APC 基因(腺瘤性息肉病基因)的选择性抑制剂,通过抑制胆固醇生物合成发挥细胞毒作用。 TASIN-1 代表了一种潜在的治疗策略,用于预防和干预具有突变 APC 的 CRC。
  5. GC17778 TAME TAME 是后期促进复合物/环体(APC/C 或 APC)的抑制剂,它与 APC/C 结合并阻止其被 Cdc20 和 Cdh1 激活,产生有丝分裂停滞。 TAME 不具有细胞渗透性。
  6. GA11219 Tos-Arg-OMe·HCl Tos-Arg-OMe.HCl 是后期促进复合物/环体(APC/C 或 APC)的抑制剂,它与 APC/C 结合并阻止其被 Cdc20 和 Cdh1 激活,产生有丝分裂停滞。 Tos-Arg-OMe.HCl 不具有细胞渗透性。

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