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509105 STAT3/STAT5 Dual Inhibitor, SH-4-54 - Calbiochem

509105
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₉H₂₇F₅N₂O₅S

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      Description
      OverviewA cell-permeable BP-1-102 (Cat. no. 573132) analog that targets STAT3 and STAT5 with comparable affinity and is 4-fold more potent in competing against phosphopeptide for binding SH2 domain of STAT3 over STAT1, exhibiting little potency against upstream kinases or the activation of 21 GPCRs, and displaying much reduced or no affinity toward other kinases in a 101-panel screen. Selectively inhibits cellular STAT3 Y705, but not S727, phosphorylation (0.5 to 5 µM) and is a more potent anticancer agent than BP-1-102 against gliobalstoma (GMB) patients-derived brain tumor stem cell (BTSC) in cultures (IC50 from 42 to 530 nM). Reported to penetrate blood-brain-barrier in mice and effectively inhibit BT73 glioma proliferation in xenografted murine brain (10 mg/kg/d via i.p.; 4 d on/ 3 d off) in vivo.
      Catalogue Number509105
      Brand Family Calbiochem®
      SynonymsSH-04-54, SH0454, SH454, 4-(N-(4-Cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)benzoic acid, STAT5 Inhibitor IV, STAT3 Inhibitor XIX
      References
      ReferencesHaftchenary, S., et al. 2013. ACS Med. Chem. Lett. 4, In press.
      Product Information
      FormWhite powder
      Hill FormulaC₂₉H₂₇F₅N₂O₅S
      Chemical formulaC₂₉H₂₇F₅N₂O₅S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSTAT3
      Secondary targetSTAT5
      Purity≥94% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      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

      STAT3/STAT5 Dual Inhibitor, SH-4-54 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      STAT3/STAT5 Dual Inhibitor, SH-4-54 - Calbiochem Certificates of Analysis

      TitleLot Number
      509105

      References

      Reference overview
      Haftchenary, S., et al. 2013. ACS Med. Chem. Lett. 4, In press.
      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.

      Revision21-February-2014 JSW
      SynonymsSH-04-54, SH0454, SH454, 4-(N-(4-Cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)benzoic acid, STAT5 Inhibitor IV, STAT3 Inhibitor XIX
      DescriptionA cell-permeable, salicyclic-to-benzoic acid-substituted BP-1-102 (Cat. no. 573132) analog that targets STAT3 and STAT5 with comparable affinity (koff/kon = KD = 300 and 464 nM, respectively) and is 4-fold more potent in competing against phosphopeptide for binding to SH2 domain of STAT3 over STAT1 (Ki = 23.5 and 92.3 µM, respectively; [phosphopeptide] = 10 nM), exhibiting little potency against the kinase activity of upstream kinases (Akt1, Erk1, JAK1/2, c-Src) or the activation of 21 GPCRs, and displaying much reduced or no affinity toward other kinases in a 101-panel screen. Selectively inhibits cellular STAT3 Y705, but not S727, phosphorylation (0.5 to 5 µM) and is a more potent anticancer agent than BP-1-102 against gliobalstoma (GMB) patients-derived brain tumor stem cell (BTSC) cultures (IC50 from 42 to 530 nM). Reported to penetrate blood-brain-barrier in mice (Conc in brain = 313 nM 30 min post 10 mg/kg i.p. dosing) and effectively inhibit BT73 glioma proliferation in xenografted murine brain via apoptosis induction (10 doses: 10 mg/kg i.p., 4 d on/ 3 d off) in vivo.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₉H₂₇F₅N₂O₅S
      Structure formulaStructure formula
      Purity≥94% 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
      ReferencesHaftchenary, S., et al. 2013. ACS Med. Chem. Lett. 4, In press.