681685 WP1130 - Calbiochem

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

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

Synonyms: Degrasyn

681685
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉H₁₈BrN₃O

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      681685-10MG
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          		 Glass bottle 10 mg
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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
          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

          Documentation

          WP1130 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          WP1130 - 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
          Chemical formulaC₁₉H₁₈BrN₃O
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          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.
          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.