500511 Histone Acetyltransferase Inhibitor VIII, NU9056 - Calbiochem

500511
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₆H₄N₂S₄

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      Description
      OverviewA cell-permeable disulfane compound that is reported to be more potent against KAT5/Tip60 than PCAF, p300, and GCN5 in cell-free HAT activity assays (IC50 ≤2, ≤36, ≤60, and >100 µM, respectively) and effectively reduce H3K14, H4K8, H4K16, but not α-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 µM). Shown to induce cell cycle arrest and apoptosis (17 to 24 µM) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI50 from 7.5 to 27 µM).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number500511
      Brand Family Calbiochem®
      Synonyms1,2-Bis(isothiazol-5-yl)disulfane, 1,2-di(isothiazol-5-yl)disulfane, KAT5 Inhibitor I, Tip60 Inhibitor I, HAT Inhibitor VIII, p300/CBP Inhibitor VII, PCAF Inhibitor V
      References
      ReferencesCoffey, K., et al. 2012. PLoS One. 7, e45539.
      Product Information
      FormYellowish-brown oil
      Hill FormulaC₆H₄N₂S₄
      Chemical formulaC₆H₄N₂S₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetKAT5
      Purity≥97% 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 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 3 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Histone Acetyltransferase Inhibitor VIII, NU9056 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Coffey, K., et al. 2012. PLoS One. 7, e45539.

      Technical Info

      Title
      White Paper - The Message in the Marks: Deciphering Cancer Epigenetics (EMD)
      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.

      Revision30-August-2013 JSW
      Synonyms1,2-Bis(isothiazol-5-yl)disulfane, 1,2-di(isothiazol-5-yl)disulfane, KAT5 Inhibitor I, Tip60 Inhibitor I, HAT Inhibitor VIII, p300/CBP Inhibitor VII, PCAF Inhibitor V
      DescriptionA cell-permeable disulfane compound that is reported to be more potent against KAT5/Tip60 than PCAF, p300, and GCN5 in cell-free HAT activity assays (IC50 ≤2, ≤36, ≤60, and >100 µM, respectively) and effectively reduce H3K14, H4K8, H4K16, but not α-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10 µM; 2 µM TSA, Cat. No. 647925, added in the last 4 h of 6 h NU9056 treatment to block HDAC activity). Shown to induce cell cycle arrest (% subG1 population after 24 h/48 h/72 h/ 96 h/dose = 9.3%/15%/22%/61%/17 µM and 12%/23%/25%/92%/24 µM) and apoptosis (fold caspase-9 cleavage increase/dose in 24 h = 2.5/17 µM & 3.5/24 µM; fold caspase-3 cleavage increase/dose in 96 h = 6.3/17 µM & 11/24 µM) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI50 in three doubling time = 7.5, 12, 16, 24, and 27 µM, respectively, against WR22rvl, LNCaP-CdxR, LNCaP-AI, LNCaP, and PC3 cells).
      FormYellowish-brown oil
      Chemical formulaC₆H₄N₂S₄
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesCoffey, K., et al. 2012. PLoS One. 7, e45539.