b-AP15 | NSC 687852 | UCHL5/Usp14 Inhibitor | AmBeed-信号通路专用抑制剂

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b-AP15 98%

货号：A619221 同义名： NSC 687852

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.

b-AP15 化学结构
CAS号：1009817-63-3

b-AP15 3D分子结构
CAS号：1009817-63-3

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b-AP15 纯度/质量文件产品仅供科研

货号：A619221 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

DUB 亚型比较
蛋白酶体亚型比较

产品名称	DUB ↓ ↑	UCH ↓ ↑	USP/UBP ↓ ↑	其他靶点	纯度
PR-619	+ Plpro, EC50: 14.2 μM	+++ UCH-L5, EC50: 12.8 μM UCH-L3, EC50: 2.95 μM	+++ USP28, EC50: 6.24 μM USP5, EC50: 4.90 μM		99%+
Degrasyn	✔			Bcr-Abl	98+%
VLX1570	+ DUB, IC50: ~10 μM				99%+
ML-323	++++ USP1-UAF1, IC50: 76 nM				99%+
LDN-57444		++++ UCH-L1, IC50: 0.4 μM UCH-L3, IC50: 25 μM			99%+
TCID		++++ UCH-L3, IC50: 0.6 μM			98%
b-AP15		+++ UCHL5, IC50: 2.1 μM			98%
P 22077			++ USP7, IC50: 8.6 μM USP47, EC50: 8.74 μM		99%+
P005091			++ USP7, EC50: 4.2 μM USP47, IC50: 4.3 μM		99+%
IU1			++ USP14, IC50: 4.7 μM		98%
NSC632839			+ USP7, EC50: 37 μM USP2, EC50: 45 μM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	20S proteasome ↓ ↑	Proteasome ↓ ↑	纯度
Ixazomib	++++ 20S proteasome, Ki: 0.93 nM 20S proteasome, IC50: 3.4 nM		99%+
Delanzomib	+++ Chymotrypsin-like proteasome, IC50: 3.8 nM		98%
Celastrol	+ 20S proteasome, IC50: 2.5 μM		98%
MLN9708	+++ 20S proteasome, Ki: 0.93 nM 20S proteasome, IC50: 3.4 nM		99%
Bortezomib	++++ 20S proteasome, Ki: 0.6 nM		98%
Oprozomib	++ 20S proteasome LMP7, IC50: 82 nM 20S proteasome β5, IC50: 36 nM		99%+
Epoxomicin	✔		99%
PI-1840	++ Chymotrypsin-like proteasome, IC50: 27 nM		98%
VR23		+++ Chymotrypsin-like proteasomes, IC50: 3 μM Trypsin-like proteasomes, IC50: 1 nM	98%
Carfilzomib		++ Proteasome, IC50: 5 nM	98%
(R)-MG-132		+ Proteasome, IC50: 100 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

b-AP15 生物活性

靶点	UCH UCHL5, IC50:2.1 μM
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].

b-AP15 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
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
human HSC2		Cytotoxicity assay		Cytotoxicity against human HSC2 by MTT method, CC50=0.094 μM	17499885

b-AP15 动物研究

Dose	Mice: 2.5 mg/kg, 5 mg/kg^[3] (i.p.)
Administration	i.p.

b-AP15 参考文献

[1]Lopez-Castejon G, Luheshi NM, et al. Deubiquitinases regulate the activity of caspase-1 and interleukin-1β secretion via assembly of the inflammasome. J Biol Chem. 2013 Jan 25;288(4):2721-33.

[2]D'Arcy P, Brnjic S, et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat Med. 2011 Nov 6;17(12):1636-40.

[3]Wang X, D'Arcy P, Caulfield TR, Paulus A, Chitta K, Mohanty C, Gullbo J, Chanan-Khan A, Linder S. Synthesis and evaluation of derivatives of the proteasome deubiquitinase inhibitor b-AP15. Chem Biol Drug Des. 2015 Nov;86(5):1036-48.

[4]Feng X, Holmlund T, Zheng C, Fadeel B. Proapoptotic effects of the novel proteasome inhibitor b-AP15 on multiple myeloma cells and natural killer cells. Exp Hematol. 2014 Mar;42(3):172-82.

[5]Tian Z, D'Arcy P, Wang X, Ray A, Tai YT, Hu Y, Carrasco RD, Richardson P, Linder S, Chauhan D, Anderson KC. A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistance. Blood. 2014 Jan 30;123(5):706-16.

[6]D'Arcy P, Brnjic S, Olofsson MH, Fryknäs M, Lindsten K, De Cesare M, Perego P, Sadeghi B, Hassan M, Larsson R, Linder S. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat Med. 2011 Nov 6;17(12):1636-40.

[7]D'Arcy P, Linder S. Proteasome deubiquitinases as novel targets for cancer therapy. Int J Biochem Cell Biol. 2012 Nov;44(11):1729-38.

b-AP15 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.92mL

2.38mL

1.19mL

23.84mL

4.77mL

2.38mL

b-AP15 技术信息

CAS号	1009817-63-3
分子式	C₂₂H₁₇N₃O₆
分子量	419.387

别名	NSC 687852
运输	蓝冰

存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 18 mg/mL(42.92 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

4% DMSO+corn oil 1 mg/mL

b-AP15 98%

b-AP15 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

b-AP15 质控信息

b-AP15 生物活性

b-AP15 细胞研究

b-AP15 动物研究

b-AP15 参考文献

b-AP15 实验方案

b-AP15 技术信息

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b-AP15 98%

b-AP15 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

b-AP15 质控信息

b-AP15 生物活性

b-AP15 细胞研究

b-AP15 动物研究

b-AP15 参考文献

b-AP15 实验方案

b-AP15 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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b-AP15 纯度/质量文件产品仅供科研