製品番号: HY-13264

Degrasyn

(別名: WP1130)

21 Cited Publications

カスタマーレビュー

Based on 21 publication(s) in Google Scholar

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.

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純度: 99.70%
CAS 番号: 856243-80-6
分子式: C₁₉H₁₈BrN₃O
分子量:384.27

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Degrasyn 構造式

CAS 番号: 856243-80-6

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数量

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (21)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

IC50: 1.8 μM (Bcr-Abl, in K562, BV-173 cells)^[1]
Deubiquitinase^[2]

Deubiquitinase アイソフォーム固有の製品をすべて表示 :

Bcr-Abl アイソフォーム固有の製品をすべて表示 :

Abl
Bcr-Abl

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]

体外実験

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].

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

体内実験

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].

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

化学情報

CAS 番号 856243-80-6
性状 Solid
分子量 384.27
分子式 C₁₉H₁₈BrN₃O
Color Light yellow to yellow
SMILES

BrC1=CC=CC(/C=C(C(N[C@H](C2=CC=CC=C2)CCC)=O)\C#N)=N1
別名

WP1130
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (21)

All Cell Proliferation/Viability AssayWBIFIn Vivo Efficacy StudyCell Imaging/Staining

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Journal Impact Factor

Nat Commun

USP2 inhibition unleashes CD47-restrained phagocytosis and enhances anti-tumor immunity. [Abstract]

2025 May 16;16(1):4564. PMID: 40379682
Nat Commun

The adaptor protein AP-3β disassembles heat-induced stress granules via 19S regulatory particle in Arabidopsis. [Abstract]

2025 Feb 27;16(1):2039. PMID: 40016204
J Adv Res

Sirtuin 7-mediated deacetylation of hypoxia-inducible factor 1-alpha facilitates glycolytic reprogramming and inflammation of keratinocytes in psoriasis. [Abstract]

2026 Apr 14:S2090-1232(26)00343-7. PMID: 41985670
Sci Adv

The cohesin-associated protein Pds5A governs the meiotic spindle assembly via deubiquitination of Kif5B in oocytes. [Abstract]

2025 Apr 11;11(15):eadt6159. PMID: 40215310
Cancer Lett

Ablation of EWS-FLI1 by USP9X inhibition suppresses cancer cell growth in Ewing sarcoma. [Abstract]

2023 Jan 1:552:215984. PMID: 36330954
Cell Death Dis

The deubiquitinase USP9X and E3 ligase WWP1 orchestrate IGF2BP2 ubiquitination homeostasis to drive TNBC progression and cisplatin sensitivity. [Abstract]

2025 Oct 6;16(1):703. PMID: 41053085

Degrasyn purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Oct 6;16(1):703. [Abstract]

Degrasyn (WP1130) (1 μM) significantly inhibit the proliferation rate and clone formation ability of TNBC cells at relatively low concentrations.

Degrasyn purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Oct 6;16(1):703. [Abstract]

The single Degrasyn (WP1130) (30 mg/kg) group, the single cisplatin group, and the WP1130 and Cisplatin drug combination group can inhibit the growth of tumor volume.
Cell Commun Signal

USP9X-mediated deubiquitination of Raptor contributes to autophagy impairment and memory deficits in P301S mice. [Abstract]

2024 Oct 24;22(1):516. PMID: 39449082

Degrasyn purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Oct 24;22(1):516. [Abstract]

HEK293T-P301S cells treated with 5 µM Degrasyn (WP1130) for 24 h. The effects of WP1130 were reversed by overexpression of Raptor or treatment with CQ.

Degrasyn purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Oct 24;22(1):516. [Abstract]

Representative fluorescence microscopy images showing the effect of 5 µM Degrasyn (WP1130) treatment for 24 h on tau protein expression in HEK293T-Tau cells along with the corresponding quantitative analysis.
Br J Pharmacol

Chicoric acid exerts therapeutic effects in DSS-induced ulcerative colitis by targeting the USP9X/IGF2BP2 axis. [Abstract]

2024 Oct 22. PMID: 39435543
JACC Basic Transl Sci

Ubiquitin Specific Protease 9X Regulates the Activation of ARK5 and Promotes Progression of Fibrotic Remodeling. [Abstract]

2025 Jul;10(7):101255. PMID: 40310323
Cell Rep

Interplay between protein acetylation and ubiquitination controls MCL1 protein stability. [Abstract]

2021 Nov 9;37(6):109988. PMID: 34758305
J Med Chem

Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. [Abstract]

2022 Oct 27;65(20):13645-13659. PMID: 36221183
Biochem Pharmacol

Deubiquitinase USP5 promotes acute myeloid leukemia through C2CD5 stabilization and PI3K/AKT/mTOR/HIF-1α-driven glycolysis. [Abstract]

2026 Feb:244:117591. PMID: 41344512
Invest Ophthalmol Vis Sci

TBK1 Knockdown Alleviates Axonal Transport Deficits in Retinal Ganglion Cells Via mTORC1 Activation in a Retinal Damage Mouse Model. [Abstract]

2023 Jul 3;64(10):1. PMID: 37395713

Degrasyn purchased from MedChemExpress. Usage Cited in: Invest Ophthalmol Vis Sci. 2023 Jul 3;64(10):1. [Abstract]

Immunofluorescent staining of RAPTOR in mouse retina following TBK1 knockdown with or without Degrasyn (40 mg/kg, i.p.) treatment after AOHT, nuclei were detected by DAPI staining.
J Cell Physiol

Deubiquitinating enzyme USP9X regulates metastasis and chemoresistance in triple-negative breast cancer by stabilizing Snail1. [Abstract]

2022 Jul;237(7):2992-3000. PMID: 35506169
J Biol Chem

Deubiquitinase USP9X stabilizes RNA m6A demethylase ALKBH5 and promotes acute myeloid leukemia cell survival. [Abstract]

2023 Aug;299(8):105055. PMID: 37454738
Pflugers Arch

Unlocking the potential: unveiling tyrphostins with Michael-reactive cyanoacrylate motif as promising inhibitors of human 5-lipoxygenase. [Abstract]

2024 Dec;476(12):1913-1928. PMID: 39347835
Oncol Lett

USP5 promotes tumor progression by stabilizing SLUG in bladder cancer. [Abstract]

2024 Sep 27;28(6):572. PMID: 39397799
Cell J

High Expression of G9a Induces Cisplatin Resistance in Hepatocellular Carcinoma. [Abstract]

2023 Feb 1;25(2):118-125. PMID: 36840458
bioRxiv

2025 May 14.
bioRxiv

2024 Nov 06.
Res Sq

2022 Jun 3.

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (260.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6023 mL

13.0117 mL

26.0234 mL

5 mM

0.5205 mL

2.6023 mL

5.2047 mL

10 mM

0.2602 mL

1.3012 mL

2.6023 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

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].

MedChemExpress (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.

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
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取扱説明書 (2659 KB)

参考文献

[1]. Bartholomeusz GA, 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

Keywords

Degrasyn

21 Cited Publications

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Degrasyn

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Ubiquitination Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Blood Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Cysteine Targeted Covalent Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 Degrasyn

Deubiquitinase アイソフォーム固有の製品をすべて表示

Bcr-Abl アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (21)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Degrasyn 関連分類

HY-13264 関連分類