Apcin

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Chemical Structure| 300815-04-7 同义名 : -
CAS号 : 300815-04-7
货号 : A1012823
分子式 : C13H14Cl3N7O4
纯度 : 98%+
分子量 : 438.654
MDL号 : MFCD00525727
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(273.56 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • E3 Ligase
描述 Apcin, a ligand for Cdc20, is a potent, competitive inhibitor of APC/C(Cdc20) Apcin competitively inhibits APC/C-dependent ubiquitination by binding to Cdc20 and preventing substrate recognition. Apcin occupies the D-box binding pocket flanking the WD40 structural domain, which prolongs mitosis[1][2][3].At concentrations of 25-50 μM for 48 hours, Apcin in combination with proTAME (6, 12 μM) significantly increases MM apoptosis[3].At 25 μM concentration, acting for 2-14 hours, Apcin induces slippage at a slower rate[2].In the concentration range of 50-200 μM, Apcin most effectively stabilises cycB1-NT and securin, with a slightly weaker effect on full-length cyclin B1[1].In the concentration range of 1.5-200 μM for 18 hours, Apcin acts synergistically with proTAME, a cell-permeable TAME prodrug, to prolong the mitotic duration of RPE1 cells[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.40mL

2.28mL

1.14mL

22.80mL

4.56mL

2.28mL
参考文献

[1]Katharine L Sackton, et al. Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C. Nature. 2014 Oct 30;514(7524):646-9.

[2]Katherine V Richeson, et al. Paradoxical mitotic exit induced by a small molecule inhibitor of APC/C Cdc20. Nat Chem Biol. 2020 May;16(5):546-555.

[3]Susanne Lub, et al. Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiple myeloma cells. Oncotarget. 2016 Jan 26;7(4):4062-76.