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B-AP15

CAS号

1009817-63-3

分子式

C22H17N3O6

主要靶点

Apoptosis|DUB

仅限科研使用

Cat No : CM03802

Print datasheet

Synonyms

DUBs|Deubiquitinase|inhibit|B AP15|BAP15|B-AP15|b-AP15|B-AP-15|Apoptosis|Inhibitor|NSC 687852|NSC687852|NSC-687852|UCH-L5

验证数据展示

  • CAS No.: 1009817-63-3

    B-AP15
    CAS#: 1009817-63-3

产品信息

CAS号 1009817-63-3
分子式 C22H17N3O6
主要靶点 Apoptosis|DUB
主要通路 细胞周期|泛素化|DNA 损伤和修复|凋亡
分子量 419.39
纯度 98%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 DUBs|Deubiquitinase|inhibit|B AP15|BAP15|B-AP15|b-AP15|B-AP-15|Apoptosis|Inhibitor|NSC 687852|NSC687852|NSC-687852|UCH-L5

靶点活性

UCHL5:2.1 μM

体内活性

作为UPS抑制剂,通过诱导cathepsin-D依赖性的溶酶体凋亡途径,B-AP15可诱导细胞死亡。与外周血单核细胞或永生化上皮细胞（hTERT-RPE1）相比,B-AP15对HCT-116细胞毒性更大。B-AP15剂量依赖性地使UbG76V-YFP受体累积（IC50：0.8 μM）,表明损伤的蛋白酶体降解受损。作用于人类结肠癌HCT-116细胞时,B-AP15（1 μM）可使多聚泛素化蛋白快速累积。B-AP15（1 μM）对ATP诱导的IL-1β从脂多糖诱导的腹腔巨噬细胞中释放有抑制作用。作用于THP-1细胞,B-AP15（1 μM）可使尼日利亚菌素诱导的细胞死亡水平降低。B-AP15（1 μM）处理脂多糖诱导的THP-1细胞,可使尼日利亚菌素处理后形成的ASC斑点数量显著减少。作用于HCT-116细胞,B-AP15（1 μM）使细胞周期在G2/M期停滞,并造成细胞周期抑制剂累积。作用于HCT-116细胞, B-AP15（2.2 μM）使细胞周期蛋白依赖性激酶CDKN1A和CDKNIB,及肿瘤抑制基因TP53的数量剂量依赖性地提高,但不影响鸟氨酸脱羧酶1的数量。

体外活性

在HCT-116结肠癌移植瘤的小鼠中,B-AP15（5 mg/kg）可使肿瘤发病显著延缓.对携带鳞状细胞癌移植瘤的重症联合免疫缺陷小鼠,B-AP15（5 mg/kg）可产生显著的抗肿瘤活性.

溶解度

DMSO:1 mg/ml

细胞实验

b-AP15 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. Cell viability is monitored by either the fluorometric microculture cytotoxicity assay or the MTT assay. For the MTT assay, cells are seeded into 96-well flat-bottomed plates overnight and exposed to drugs, using DMSO as the control. At the end of incubations, 10 μl of a stock solution of 5 mg/mL MTT is added into each well, and the plates are incubated 4 hours at 37°C. Formazan crystals are dissolved with 100 μL 10% SDS/10 mM HCl solution overnight at 37°C. Absorbance is measured using an enzyme-linked immunosorbent assay (ELISA) plate reader at 590 nm[2].

参考文献

1.D'Arcy P, et al. Nat Med. 2011, 17(12):1636-40.
2.D'Arcy P, et al. Int J Biochem Cell Biol. 2012, 44(11):1729-38.
3.Lopez-Castejon G, et al. J Biol Chem, 2013, 288(4), 2721-2733.

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