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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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681685
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
856243-80-6C₁₉H₁₈BrN₃O

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681685-10MGCN
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      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.