2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  3. Deubiquitinase Bcr-Abl Autophagy Apoptosis
  4. Degrasyn

Degrasyn  (Synonyms: WP1130)

目录号: HY-13264 纯度: 99.70%
COA 产品使用指南

摩尔计算器

Degrasyn (WP1130) 是可渗透细胞的 去泛素化酶(DUB) 抑制剂，直接抑制USP9x，USP5，USP14和UCH37的DUB活性。 Degrasyn 减弱抗细胞凋亡蛋白 Bcr-Abl 和 JAK2。

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Degrasyn Chemical Structure

Degrasyn Chemical Structure

CAS No. : 856243-80-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥715
In-stock
1 mg ￥295
In-stock
5 mg ￥650
In-stock
10 mg ￥1150
In-stock
25 mg ￥2588
In-stock
50 mg ￥4399
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Degrasyn 相关抗体

Top Publications Citing Use of Products

查看 Deubiquitinase 亚型特异性产品:

查看所有亚型
USP1 USP2 USP7 USP8 USP30 UCHL1

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.

IC50 & Target

IC50: 1.8 μM (Bcr-Abl, in K562, BV-173 cells)[1]
Deubiquitinase[2]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
1.7 μM
Compound: WP1130
Cytotoxicity against human A375 cells after 72 hrs by MTT assay
Cytotoxicity against human A375 cells after 72 hrs by MTT assay
[PMID: 24457091]
K562 IC50
2.4 μM
Compound: WP1130
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
[PMID: 24457091]
MM1.S IC50
1.2 μM
Compound: WP1130
Cytotoxicity against human MM1S cells after 72 hrs by MTT assay
Cytotoxicity against human MM1S cells after 72 hrs by MTT assay
[PMID: 24457091]
U-266 IC50
1.3 μM
Compound: WP1130
Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay
[PMID: 22036213]
体外研究
(In Vitro)

Degrasyn, a small molecule that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. Degrasyn is more effective in inducing apoptosis of myeloid and lymphoid tumor cells (IC50 0.5 to 2.5 μM) than normal CD34+ hematopoietic precursors, dermal fibroblasts, or endothelial cells (IC50 ~5 to 10 μM). Degrasyn reduces Bcr/Abl protein levels through a unique mechanism that is not affected by mutations that interfere with imatinib mesylate binding. Degrasyn inhibits phosphorylation of both the wild-type and the T315I mutant Bcr/Abl proteins, as demonstrated by the rapid disappearance (within 1 hour) of phosphotyrosyl-Bcr/Abl in both BV173 and BV173R cells. Degrasyn-induced down-regulation of Bcr/Abl is accompanied by apoptosis of CML cells[1]. Treatment with Degrasyn yields an anti-proliferative effect across all cell lines tested in a dose-dependent manner. Notably, treatment with Degrasyn results in marked anti-proliferative activity and morphological changes in NCH644 and NCH421K glioma stem-like cells. Treatment with Degrasyn results in a dose-dependent and probably compensatory increase of Mcl-1 mRNA levels after 6 h and only a minor decrease after 24 h. Similar findings are observed for Usp9X levels. These data suggest that Degrasyn down-regulates Mcl-1 and Usp9X through a post-transcriptional mechanism[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Degrasyn 相关抗体:
体内研究
(In Vivo)

Degrasyn suppresses the growth of K562 heterotransplanted tumors as well as both wild-type Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice. To assess the possible therapeutic activity of Degrasyn against CML, nude mice received a subcutaneous transplant with K562 cells and are treated with 30 mg/kg Degrasyn every other day for 9 days after palpable tumor formation (10 days). This dose and schedule are well tolerated and effective in other tumor models. Antitumor activity is compared with that after daily Imatinib mesylate treatment (50 mg/kg). Nineteen days after tumor inoculation, tumors in the control group reached maximum allowable dimension, and the effect of therapy is assessed. Degrasyn treatment suppresses K562 tumor growth to an extent comparable to that observed in imatinib mesylate-treated animals, suggesting that Degrasyn is active in reducing the growth of established K562 tumors[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

384.27

Formula

C19H18BrN3O
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (260.23 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6023 mL 13.0117 mL 26.0234 mL
5 mM 0.5205 mL 2.6023 mL 5.2047 mL
查看完整储备液配制表

* 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.51 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.51 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.70%

COA (191 KB) HNMR (337 KB) LCMS (136 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

CML cells are seeded in 96-well plates (2×104 cells/well) and Degrasyn, Imatinib mesylate, or Dasatinib (0.08-10 μM) are added in a final volume of 100 μL medium. Plates are incubated at 37°C for 72 hours, after which 20 μL of MTT reagent (stock 5 mg/mL) is added, and the plates are incubated at 37°C for another 2 hours. Cells are lysed with 100 μL lysis buffer (20% SDS in 50% N, N-dimethylformamide adjusted to pH 4.7 with 80% acetic acid and 1 M hydrochloric acid; final concentration of acetic acid is 2.5% and hydrochloric acid is 2.5%) and incubated for 6 hours. The optical density of each sample at 570 nm is determined with a SPECTRA MAX M2 plate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
To assess activity against T315I Bcr/Abl mutant cells, BaF/3 cells transfected with wild-type Bcr/Abl or the T315I mutant are transplanted into female Swiss nude mice (5-6 weeks old). BaF/3wt cells are suspended (5×107 cells/mL) in RPMI medium, and 0.1 mL of this suspension is injected intravenously into 10 mice. The same procedure is used to inoculate 10 mice with BaF/3/T315I cells. One day after tumor cell inoculation, mice are randomly assigned to 1 of 3 groups: one group received Degrasyn (40 mg/kg, intraperitoneally) in 50 μL DMSO/PEG300 (vehicle) every other day (7 injections); another received imatinib mesylate (100 mg/kg, intraperitoneally) in vehicle daily (14 injections); and the third received vehicle alone daily (14 injections). Spleens from each mouse are harvested, photographed, and weighed 15 days after tumor cell inoculation.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Degrasyn 相关分类

完整储备液配制表

* 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6023 mL 13.0117 mL 26.0234 mL 65.0584 mL
5 mM 0.5205 mL 2.6023 mL 5.2047 mL 13.0117 mL
10 mM 0.2602 mL 1.3012 mL 2.6023 mL 6.5058 mL
15 mM 0.1735 mL 0.8674 mL 1.7349 mL 4.3372 mL
20 mM 0.1301 mL 0.6506 mL 1.3012 mL 3.2529 mL
25 mM 0.1041 mL 0.5205 mL 1.0409 mL 2.6023 mL
30 mM 0.0867 mL 0.4337 mL 0.8674 mL 2.1686 mL
40 mM 0.0651 mL 0.3253 mL 0.6506 mL 1.6265 mL
50 mM 0.0520 mL 0.2602 mL 0.5205 mL 1.3012 mL
60 mM 0.0434 mL 0.2169 mL 0.4337 mL 1.0843 mL
80 mM 0.0325 mL 0.1626 mL 0.3253 mL 0.8132 mL
100 mM 0.0260 mL 0.1301 mL 0.2602 mL 0.6506 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Degrasyn856243-80-6WP1130WP 1130WP-1130DeubiquitinaseBcr-AblAutophagyApoptosisDUBsInhibitorinhibitorinhibit

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