Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

681685 WP1130 - CAS 856243-80-6 - Calbiochem

A cell-permeable tyrphostin compound that acts as a partially selective deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway.

WP1130 - CAS 856243-80-6 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

同义词: Degrasyn

681685
Purchase on Sigma-Aldrich

概述

Replacement Information

重要规格表

CAS #Empirical Formula
856243-80-6C₁₉H₁₈BrN₃O

Products

产品目录编号包装 数量 / 包装
681685-10MGCN 玻璃瓶 10 mg
Description
OverviewA cell-permeable tyrphostin compound that acts as a partially selective deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway. Reported to cause accumulation of polyubiquitinated p53, JAK2 and Bcr-Abl, and reduce c-Myc and MCL-1 protein levels in several tumor cells and downregulate Stat3 and NF-κB activities (IC50 < 1 µM in MCL cells) leading to tumor cell apoptosis (IC50 ~1.2 µM in Z138 cells). Suggested to modify active site cysteine of DUB and inhibit USP5, UCH-L1, USP9x, USP14, and UCH37 activities (≥80% inhibition at 5 µM) without affecting 20S proteasome. Reported to exert stronger antiproliferative and antitumor properties than STAT3 Inhibitor III, WP1066 (Cat. No. 573097) in xenograft mouse models of CML and melanoma.
Catalogue Number681685
Brand Family Calbiochem®
SynonymsDegrasyn
References
ReferencesKapuria, V., et al. 2010. Cancer Res. 70, 9265.
Pham, L.V., et al. 2010. Mol. Cancer Ther. 9, 2026.
Bartholomeusz, G.A, et al. 2007. Cancer Res. 67, 3912.
Bartholomeusz, G.A, et al. 2007. Blood 109, 3470.
Product Information
CAS number856243-80-6
FormLight yellow solid
Hill FormulaC₁₉H₁₈BrN₃O
Chemical formulaC₁₉H₁₈BrN₃O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
产品目录编号 GTIN
681685-10MGCN 04055977225273

Documentation

WP1130 - CAS 856243-80-6 - Calbiochem MSDS

职位

物料安全数据表 (MSDS) 

WP1130 - CAS 856243-80-6 - Calbiochem 分析证书

标题批号
681685

参考

参考信息概述
Kapuria, V., et al. 2010. Cancer Res. 70, 9265.
Pham, L.V., et al. 2010. Mol. Cancer Ther. 9, 2026.
Bartholomeusz, G.A, et al. 2007. Cancer Res. 67, 3912.
Bartholomeusz, G.A, et al. 2007. Blood 109, 3470.
数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision02-April-2012 JSW
SynonymsDegrasyn
DescriptionA cell-permeable tyrphostin compound that acts as a partially selective deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway. Reported to cause accumulation of polyubiquitinated p53, JAK2 and Bcr-Abl, and reduce c-Myc and MCL-1 protein levels in several tumor cells and downregulate Stat3 and NF-κB activities (IC50 < 1 µM in MCL cells) leading to tumor cell apoptosis (IC50 ~1.2 µM in Z138 cells). Suggested to modify active site cysteine of DUB and inhibit USP5, UCH-L1, USP9x, USP14, and UCH37 activities (≥80% inhibition at 5 µM) without affecting 20S proteasome. Reported to exert stronger antiproliferative and antitumor properties than STAT3 Inhibitor III, WP1066 (Cat. No. 573097) in xenograft mouse models of CML and melanoma.
FormLight yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number856243-80-6
Chemical formulaC₁₉H₁₈BrN₃O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesKapuria, V., et al. 2010. Cancer Res. 70, 9265.
Pham, L.V., et al. 2010. Mol. Cancer Ther. 9, 2026.
Bartholomeusz, G.A, et al. 2007. Cancer Res. 67, 3912.
Bartholomeusz, G.A, et al. 2007. Blood 109, 3470.