506071 | InSolution™ I-BET - CAS 1260907-17-2 - Calbiochem

506071
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₂H₂₂ClN₅O₂ 1260907-17-2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.06071.0001
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          Glass bottle 5 mg
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          Description
          Catalogue Number506071
          Brand Family Calbiochem®
          Synonyms(S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
          References
          ReferencesNicodeme, E., et al. 2010. Nature 468, 1119.
          Product Information
          CAS number1260907-17-2
          FormLiquid
          FormulationA 50 mM (5 mg/236 µL) sterile-filtered solution of I-BET (Cat. No. 401010) in DMSO.
          Hill FormulaC₂₂H₂₂ClN₅O₂
          Chemical formulaC₂₂H₂₂ClN₅O₂
          Hygroscopic Hygroscopic
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary Targettandem bromodomains of BET
          Purity≥98% by Chiral 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 Dry Ice Only
          Toxicity Standard Handling
          Storage ≤ -70°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Avoid freeze/thaw Avoid freeze/thaw
          Do not freeze Ok to freeze
          Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots 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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Nicodeme, E., et al. 2010. Nature 468, 1119.
          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.

          Revision11-July-2014 JSW
          Synonyms(S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
          DescriptionA cell-permeable benzodiazepine compound that binds the tandem bromodomains of BET (bromodomain and extra terminal domain) family members BRD2 (1-473), BRD3 (1-434), and BRD4 (1-477) with high affinity (Kd = 61.3, 50.5, and 55.2 nM, respectively, by ITC) and effectively competes against tetra-acetylated H4 peptide (Millipore cat. no. 12-379) for BRD2/3/4 binding (IC50 = 32.5, 42,4, and 36.1 nM, respectively, in competitive equilibrium binding assays), while exhibiting little affinity toward 5 other bromodomain-containing proteins (ATAD2, BAZ2B, CREBBP, PCAF, SP140) or a panel of 38 cellular enzymes, GPCRs, transporters, and ion channels. Shown to differentially modulate LPS-induced gene expression, notably suppressing LPS-induced upregulation of genes involved in inflammatory response, in murine BMDMs (bone marrow-derived macrophages) in vitro (30 min 1 µM pretreatment) and effectively prevent LPS-, heat-killed Salmonella typhimurium-, and CLP- (caecal ligation and puncture) induced death in mice in vivo (30 mg/kg i.v.). Cellular Brd2/3/4 knockdown using siRNA results in mostly the same effect as I-BET treatment in modulating LPS gene induction profile in murine BMDMs, but not without exceptions, indicating that not all BET-dependent transcription regulations are mediated via its binding to acetylated histones.
          FormLiquid
          FormulationA 50 mM (5 mg/236 µL) sterile-filtered solution of I-BET (Cat. No. 401010) in DMSO.
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1260907-17-2
          Chemical formulaC₂₂H₂₂ClN₅O₂
          Structure formulaStructure formula
          Purity≥98% by Chiral HPLC
          Storage ≤ -70°C
          Hygroscopic
          Protect from light
          Avoid freeze/thaw
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesNicodeme, E., et al. 2010. Nature 468, 1119.