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506305 SKP2 E3 Ligase Inhibitor III - Calbiochem

506305
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₄H₂₄N₂O₃S

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable benzothiazolylchromenone compound that disrupts Skp2-Skp1 interaction via direct Skp2 affinity binding and selectively prevents Skp2-, but not Fbw7- or β-TrCP-, Skp1-Cullin-1-F-box (SFC) complex-mediated substrates ubiquitination, effectively preventing Skp2 substrates activation (Akt) and degradation (p21 & p27) with concomitant down-regulation of cellular Skp2 protein level (10 to 20 µM in HEK293T & PC3 cultures). Exhibits antiproliferation activity toward a panel of 8 cancer (IC50 from 1.22 to 10.5 µM) and reduces ALDH+ cancer stem cell population in PC3 cultures (10 to 20 µM). Exhibits good pharmacokinetic property and is efficacious in suppressing A549 and PC3 tumor growth in mice (40 to 80 mg/kg/d i.p.) in vivo.
      Catalogue Number506305
      Brand Family Calbiochem®
      Synonyms3-(1,3-Benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-chromen-4-one, 3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one, 3-Benzothiazol-2-yl-6-ethyl-7-hydroxy-8-(piperidylmethyl)chromen-4-one, p21/Cip1/CKI/Waf1 Activator III, CRL1SKP2 Inhibitor III, p27/Kip1 Activator III, S-phase Kinase-associated Protein 2 Inhibitor III, SCFSKP2 Inhibitor III, SZL-P1-41
      References
      ReferencesChan, C.H., et al. 2013 Cell 154, 556.
      Product Information
      FormBeige powder
      Hill FormulaC₂₄H₂₄N₂O₃S
      Chemical formulaC₂₄H₂₄N₂O₃S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSkp2
      Purity≥98% 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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      SKP2 E3 Ligase Inhibitor III - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Chan, C.H., et al. 2013 Cell 154, 556.
      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.

      Revision15-January-2013 JSW
      Synonyms3-(1,3-Benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-chromen-4-one, 3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one, 3-Benzothiazol-2-yl-6-ethyl-7-hydroxy-8-(piperidylmethyl)chromen-4-one, p21/Cip1/CKI/Waf1 Activator III, CRL1SKP2 Inhibitor III, p27/Kip1 Activator III, S-phase Kinase-associated Protein 2 Inhibitor III, SCFSKP2 Inhibitor III, SZL-P1-41
      DescriptionA cell-permeable benzothiazolylchromenone compound that disrupts Skp2-Skp1 interaction via direct Skp2 affinity binding and selectively prevents Skp2-, but not Fbw7- or β-TrCP-, Skp1-Cullin-1-F-box (SFC) complex-mediated substrates ubiquitination both in cell-free systems and in cultures, effectively preventing ubiquitination-dependent activation (Akt) and degradation (p21 & p27) of Skp2 substrates with concomitant down-regulation of cellular Skp2 protein level (10 to 20 µM in HEK293T & PC3 cultures). Exhibits antiproliferation activity toward a panel of 8 cancer (IC50 from 1.22 to 10.5 µM), but not normal PNT1A epithelial or IMR90 fibroblast, lines and effectively reduces ALDH+ cancer stem cell (CSC; Cancer Initiating Cell) population in prostate cancer PC3 cultures (10 to 20 µM) by promoting p53-independent senescence and blocking Akt-dependent aerobic glycolysis. Exhibits good pharmacokinetic property (tmax = 1 h; t1/2 >6 h; Cmax >1 µM/plasma and >4 µM/tumor in 200 mm3 PC3 tumor-bearing mice; 80 mg/kg i.p.) and is efficacious in suppressing A549 and PC3 tumor growth in mice (40 to 80 mg/kg/d i.p.) in vivo.
      FormBeige powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₄H₂₄N₂O₃S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (5 mg/ml). Use only fresh DMSO for reconstitution.
      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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesChan, C.H., et al. 2013 Cell 154, 556.