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505298 p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem

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Synonyme: GCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV, 4-(4-Methoxyphenylsulfonyloxyimino)-2,6-dimethyl-2,5-cyclohexadien-1-one

Primary Target: p300 HAT
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505298
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
321695-57-2C₁₅H₁₅NO₅S

Preis & Verfügbarkeit

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      		 Glasflasche 10 mg
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      Description
      OverviewA cell-permeable phenylsulfonyloxyiminocyclohexadienone compound that acts as a potent, selective, and reversible inhibitor of p300 histone acetyl transferase (IC50 = 1.98 µM). Shown to occupy Ac-CoA binding pocket of p300, and less potent to CBP, PCAF, GCN5 and GNAT. Suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. Does neither inhibit the activities of histone deacetylases 1, 6, and 11 nor 8-diverse histone methyltransferases tested (DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2). Reported to suppress tumor growth in mice bearing tumor xenografts of MDAMB-468 cell line (at 500 µg/100 µl, i.p. twice a week).
      Catalogue Number505298
      Brand Family Calbiochem®
      SynonymsGCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV, 4-(4-Methoxyphenylsulfonyloxyimino)-2,6-dimethyl-2,5-cyclohexadien-1-one
      References
      ReferencesYang, H., et al. 2013. Mol. Cancer Ther. 12, 610.
      Product Information
      CAS number321695-57-2
      FormBrown solid
      Hill FormulaC₁₅H₁₅NO₅S
      Chemical formulaC₁₅H₁₅NO₅S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetp300 HAT
      Purity≥99% 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
      Global Trade Item Number
      Bestellnummer GTIN
      5.05298.0001 04055977243666

      Documentation

      p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Yang, H., et al. 2013. Mol. Cancer Ther. 12, 610.
      Datenblatt

      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.

      Revision10-January-2014 JSW
      SynonymsGCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV, 4-(4-Methoxyphenylsulfonyloxyimino)-2,6-dimethyl-2,5-cyclohexadien-1-one
      DescriptionA cell-permeable phenylsulfonyloxyiminocyclohexadienone compound that acts as a potent, selective, and reversible inhibitor of p300 histone acetyl transferase (IC50 = 1.98 µM). Shown to occupy Ac-CoA binding pocket of p300, and less potent to CBP, PCAF, GCN5 and GNAT. Suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. Does neither inhibit the activities of histone deacetylases 1, 6, and 11 nor 8-diverse histone methyltransferases tested (DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2). Reported to suppress tumor growth in mice bearing tumor xenografts of MDAMB-468 cell line (at 500 µg/100 µl, i.p. twice a week).
      FormBrown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number321695-57-2
      Chemical formulaC₁₅H₁₅NO₅S
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesYang, H., et al. 2013. Mol. Cancer Ther. 12, 610.