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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.

Synonyms: Degrasyn

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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
856243-80-6C₁₉H₁₈BrN₃O

Products

Catalogue NumberPackaging Qty/Pack
681685-10MGCN Glass bottle 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
Catalogue Number GTIN
681685-10MGCN 04055977225273

Documentation

WP1130 - CAS 856243-80-6 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

WP1130 - CAS 856243-80-6 - Calbiochem Certificates of Analysis

TitleLot Number
681685

References

Reference overview
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.
Data Sheet

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.