Degrasyn (Synonyms: WP1130)

Name: Degrasyn
Brand: MedChemExpress
SKU: HY-13264
Rating: 5.0 (11 reviews)

Cat. No.: HY-13264 Purity: 99.70%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Degrasyn Chemical Structure

CAS No. : 856243-80-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 415	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 660	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

11 Publications Citing Use of MCE Degrasyn

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Deubiquitinase Isoform Specific Products:

View All Isoforms

USP1 USP2 USP7 USP8 USP30 UCHL1

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

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]

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].

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

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].

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

Molecular Weight

384.27

Formula

C₁₉H₁₈BrN₃O

CAS No.

856243-80-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2602 mL	1.3012 mL	2.6023 mL

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.70%

Select Batch:

Data Sheet (278 KB) SDS (420 KB)

COA (246 KB) HNMR (337 KB) LCMS (136 KB)

Handling Instructions (2659 KB)

References

[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]

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.
References	[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]

Complete Stock Solution Preparation Table

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

Degrasyn Related Classifications

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

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Degrasyn (Synonyms: WP1130)

Customer Review

Degrasyn Related Antibodies

11 Publications Citing Use of MCE Degrasyn

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Deubiquitinase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Degrasyn Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Degrasyn Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report