Apcin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEApcinCat. No.: HY-110287CAS No.: 300815-04-7分式: CHClNO分量: 438.65作靶点: APC作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 250 mg/mL (569.93 mM; Need ultrasonic)Mass

2、Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2797 mL 11.3986 mL 22.7972 mL5 mM 0.4559 mL 2.2797 mL 4.5594 mL10 mM 0.2280 mL 1.1399 mL 2.2797 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶

3、剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.74 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.74 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.74 mM); Clear solution1

4、/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 ApcinCdc20 的配体，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 结合并阻底物识别来竞争性抑制 APC/C 依赖性泛素化。Apcin 占据 WD40 结构域侧的 D-box 结合袋，并可以延长有丝分裂。体外研究 Apcin (25-50 M; 48 hours) significantly increases MM apoptosis combining with pr

5、oTAME (6, 12 M) 3.Apcin (25 M; 2-14 hours) induces slippage more slowly 2.Apcin (50-200 M) stabilizes cycB1-NT and securin most effectively, with somewhat weaker effects againstfull-length cyclin B1 1.Apcin (1.5-200 M; 18 hours) synergizes with proTAME (a cell-permeable TAME prodrug) to prolong mito

6、ticduration in RPE1 cells 1.Apoptosis Analysis 3Cell Line: HMCLs LP-1 and RPMI-8226 cellsConcentration: 25, 50 MIncubation Time: 48 hoursResult: Had minor effects on multiple myeloma (MM) cells alone and significantly increased MMapoptosis combining with proTAME (6, 12 M).Western Blot Analysis 2Cell

7、 Line: HeLa cells with Nocodazole (100nM)Concentration: 25MIncubation Time: 2-14 hoursResult: Induced slippage more slowly, as indicated by Cdc27 dephosphorylation and a reductionin cyclin B1, securin and phosphoH3 levels beginning 4-6h after mitotic entry.REFERENCES1. Katharine L Sackton, et al. Sy

8、nergistic blockade of mitotic exit by two chemical inhibitors of the APC/C. Nature. 2014 Oct30;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. 2020May;16(5):546-555.3. Susanne Lub, et al. Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiplemyeloma cells. Oncotarget. 2016 Jan 26;7(4):4062-76.McePdfHeight Caution: Product has not been fully validated for medical appli