Degrasyn | Wp1130 | Deubiquitinase Inhibitor | AmBeed-信号通路专用抑制剂

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Degrasyn {[allProObj[0].p_purity_real_show]}

货号：A535148 同义名： Wp1130

WP1130 is a selective small molecular deubiquitinase (USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and a Bcr/Abl destruction pathway activator with an IC50 of 1.8 μM for K562 cells.

Degrasyn 化学结构
CAS号：856243-80-6

Degrasyn 3D分子结构
CAS号：856243-80-6

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Degrasyn 纯度/质量文件产品仅供科研

货号：A535148 标准纯度： {[allProObj[0].p_purity_real_show]} 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: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

转化生长因子-β 亚型比较
Bcr-Abl 亚型比较
DUB 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		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	Abl ↓ ↑	Bcr-Abl ↓ ↑	其他靶点	纯度
NVP-BHG 712	+ c-Abl, IC50: 1.667 μM			99%+
KW-2449	+++ Abl (T315I), IC50: 4 nM Abl, IC50: 14 nM		FLT3	99%+
Ponatinib	++++ Abl, IC50: 0.37 nM			98%
AT9283				99%+
Imatinib Mesylate	+ v-Abl, IC50: 600 nM		c-Kit,PDGFR	99%
Danusertib	++ Abl, IC50: 25 nM		RET	99%+
Rebastinib	++++ u-Abl1 (T315I), IC50: 5 nM p-Abl1 (native), IC50: 0.75 nM		Tie-2,FLT3	99%+
PP121	++ Abl, IC50: 18 nM		PDGFR,VEGFR	99%+
GNF-7	+++ E255V, IC50: 122 nM M351T, IC50: 133 nM			99%+
Olverembatinib dimesylate	++++ Abl (G250E), IC50: 0.35 nM Abl, IC50: 0.34 nM			99%
Dasatinib monohydrate	++++ Abl , IC50: 0.6 nM		Src	98%
Dasatinib	++++ Abl, IC50: 0.6 nM		Src	98%
Bafetinib	+++ Abl, IC50: 5.8 nM			98+%
GNF-2		+ Bcr-Abl (K562 cell line), IC50: 273 nM Bcr-Abl (SUP-B15 cell line), IC50: 268 nM		98%+
Degrasyn		+ Bcr-Abl, IC50: 1.8 μM	DUB	98+%
GNF-5		++ Bcr-Abl, IC50: 220 nM		98%
Radotinib		++ BCR-ABL1, IC50: 34 nM		98+%
PD173955			Src	99%+
Nilotinib		++ Bcr-Abl, IC50: <30 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。

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	+++ USP5, EC50: 4.90 μM USP28, EC50: 6.24 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			++ USP47, IC50: 4.3 μM USP7, EC50: 4.2 μM		99+%
IU1			++ USP14, IC50: 4.7 μM		98%
NSC632839			+ USP2, EC50: 45 μM USP7, EC50: 37 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。

Degrasyn 生物活性

靶点

Bcr-Abl

Bcr-Abl, IC50:1.8 μM
DUB

描述

WP1130 is a partly selective DUB inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function. WP1130 at 5μM induced rapid accumulation of polyubiquitinated (K48/K63-linked) proteins into juxtanuclear aggresomes, without affecting 20S proteasome activity. WP1130-mediated inhibition of tumor-activated DUBs resulted in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53, in BV173 cells treated by 5μM WP1130 for 4h^[3]. WP1130 at 5μM specifically and rapidly down-regulatef both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells, not requiring the participation of the proteasomal pathway. And this loss of Bcr/Abl protein correlated with the onset of apoptosis and reduced phosphorylation of Bcr/Abl substrates, including p-Stat5 and p-Hck. It was more effective in reducing leukemic versus normal hematopoietic colony formation and strongly inhibited colony formation of cells derived from patients with T315I mutant Bcr/Abl–expressing CML in blast crisis. WP1130 suppressed the growth of K562 heterotransplanted tumors of mice treated with WP1130 at 30mg/kg, i.p., every other day for 9 days^[4].

Degrasyn 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human A375 cells		Cytotoxicity assay	72 h	Cytotoxicity against human A375 cells after 72 hrs by MTT assay, IC50=1.7 μM	24457091
human K562 cells		Cytotoxicity assay	72 h	Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=2.4 μM	24457091
human Mino cells		Cytotoxicity assay	72 h	Cytotoxicity against human Mino cells after 72 hrs by MTT assay, IC50=0.8 μM	24457091
human MM1 cells		Function assay	24 to 72 hrs	Antitumor activity against human MM1 cells after 24 to 72 hrs by MTT assay, IC50=1 μM	22036213

Degrasyn 动物研究

Dose	Mice: 20 mg/kg^[3] (i.p.), 40 mg/kg^[4] (i.p.)
Administration	i.p.

Degrasyn 参考文献

[1]Kapuria V, Peterson LF, et al. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Res. 2010 Nov 15;70(22):9265-76.

[2]Bartholomeusz GA, Talpaz M, et al. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood. 2007 Apr 15;109(8):3470-8. Epub 2007 Jan 3.

[3]Kapuria V, Peterson LF, Fang D, Bornmann WG, Talpaz M, Donato NJ. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Res. 2010 Nov 15;70(22):9265-76. doi: 10.1158/0008-5472.CAN-10-1530. Epub 2010 Nov 2. PMID: 21045142.

[4]Bartholomeusz GA, Talpaz M, Kapuria V, Kong LY, Wang S, Estrov Z, Priebe W, Wu J, Donato NJ. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood. 2007 Apr 15;109(8):3470-8. doi: 10.1182/blood-2006-02-005579. Epub 2007 Jan 3. PMID: 17202319; PMCID: PMC1852235.

Degrasyn 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.01mL

2.60mL

1.30mL

26.02mL

5.20mL

2.60mL

Degrasyn 技术信息

CAS号	856243-80-6
分子式	C₁₉H₁₈BrN₃O
分子量	384.27

别名	Wp1130
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(273.25 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

Degrasyn {[allProObj[0].p_purity_real_show]}

Degrasyn 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Degrasyn 质控信息

Degrasyn 生物活性

Degrasyn 细胞研究

Degrasyn 动物研究

Degrasyn 参考文献

Degrasyn 实验方案

Degrasyn 技术信息

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Degrasyn 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Degrasyn 质控信息

Degrasyn 生物活性

Degrasyn 细胞研究

Degrasyn 动物研究

Degrasyn 参考文献

Degrasyn 实验方案

Degrasyn 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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Degrasyn 纯度/质量文件产品仅供科研