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CAS No.: 1009817-63-3

b-AP15 Catalog No. CSN15845

Synonyms: NSC 687852;USP14 Inhibitor III;UCHL5UCH37 Inhibitor II

b-AP15 is an inhibitor of the ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5) and ubiquitin-specific-processing protease 14 (USP14). In purified 19S proteasomes, b-AP15 can inhibit DUB activity with an IC50 of 2.1 μM.

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实验方案

技术信息

生物活性

描述The ubiquitin-specific peptidases (USPs) are the main members of the deubiquitinase(DUB) family. b-AP15 is an inhibitor of 19S proteasome deubiquitinase (DUB) with IC50 value of 6.5 μM^[3]. In vitro, b-AP15 induced time- and dose-dependent apoptosis of the human multiple myeloma cell lines RPM18226 and U266. b-AP15 triggered processing of pro-caspase-3 and cleavage of ploy (ADP-ribose) polymerase in the human multiple myeloma cell. b-AP15 also induced caspase-independent apoptosis in primary human natural killer cells^[4]. In vivo, administration of b-AP15 at 4 mg/kg once daily for 14 days was well tolerated, inhibited tumor growth, and prolong survival in human multiple myeloma xenograft models^[5]. Treatment with b-AP15 at dose of 5 mg/kg inhibited tumor growth in SCID mice with FaDu human tumor xenograft and C57BL/6J mice with Lewis lung carcinomas (LLCs). Treatment with b-AP15 at dose of 2.5 mg/kg also inhibited tumor growth in BALB/c mice with orthotopic breast carcinoma. In addition, b-AP15 can inhibited organ infiltration in an acute myeloid leukemia model^[6].
作用机制b-AP15 blocks the DUB activity of the 19S regulatory particle (19S RP) without inhibiting the proteolytic activities of the 20S core particle (20S CP), and inhibits two proteasome-associated DUBs, USP14 and UCHL5, resulting in a rapid accumulation of high molecular weight ubiquitin conjugates and a functional proteasome shutdown^[7].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CEM cells	-	Cytotoxicity assay	-	Cytotoxicity against human CEM cells, IC50=0.26 μM	19819135
HL60 cells	-	Cytotoxicity assay	-	Cytotoxicity against human HL60 cells in presence of RPMI1640 containing 10% fetal bovine serum by trypan blue exclusion test, CC50=0.13 μM	17499885
HSC4 cells	-	Cytotoxicity assay	-	Cytotoxicity against human HSC4 cells by MTT method, CC50=0.56 μM	17499885

更多
动物研究
剂量
Mice: 2.5 mg/kg, 5 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 2.5 mg/kg, 5 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3844 mL
- 11.9222 mL
- 23.8443 mL
- 5 mM
- 0.4769 mL
- 2.3844 mL
- 4.7689 mL
- 10 mM
- 0.2384 mL
- 1.1922 mL
- 2.3844 mL

技术信息

CAS号

1009817-63-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H17N3O6

运输

蓝冰

分子量

419.39

别名

NSC 687852;USP14 Inhibitor III;UCHL5UCH37 Inhibitor II

溶解度

DMSO	47.0 mg/mL (112.1 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

4% DMSO+corn oil

1 mg/mL

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