533169 BET Inhibitor, I-BET726 - Calbiochem

533169
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₅H₂₃ClN₂O₃

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      5.33169.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable tetrahydroquinoline based compound that acts as a highly potent and selective inhibitor of bromodomain and extra-terminal (BET) family proteins (IC50 = 41, 31, and 22 nM for BRD2, BRD3, BRD4, respectively). Binds to the acetyl-lysine recognition pocket of BET proteins and competes with tetra-acetylated histone H4 peptides (K5ac, K8ac, K12ac, K16ac) for binding to the bromodomains of these proteins. Does not affect the activity of over 50 different receptors, ion channels, and transporters even at higher concentrations (1-10 µM). Exhibits cytotoxicity towards neuroblastoma cell lines, induces apoptosis, and inhibits their growth (gIC50 = 26 and 60 nM for CHP-212 and SK-N-AS cells, respectively). Suppresses the growth of human neuroblastoma xenografts in murine models (5 mg/kg, p.o. for 2 weeks) and reduces the expression of MYCN and BCL2. Shown to improve survival rate of Balb/c mice subjected to LPS-induced (15 - 20 mg/kg) septic shock (10 mg/kg, i.v.). Displays desirable pharmacokinetic properties (t1/2 = 3.6 h; AUC 0-t = 6.03 µg/h/ml at 10 mg/kg i.v. in mice).

          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 Number533169
          Brand Family Calbiochem®
          SynonymsBET Inhibitor, BET726, GSK1324726A, 4-((2S,4R)-1-Acetyl-4-((4-chlorophenyl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid
          References
          ReferencesGosmini, R., et al. 2014. J. Med. Chem. 57, 811.
          Wyce, A., et al. 2013. Plos One. 8, e72967.
          Product Information
          FormLight yellow solid
          Hill FormulaC₂₅H₂₃ClN₂O₃
          Chemical formulaC₂₅H₂₃ClN₂O₃
          ReversibleY
          Applications
          Biological Information
          Primary TargetBET
          Primary Target IC<sub>50</sub>41 nM, 31 nM, and 22 nM for BRD2, BRD3, BRD4, BRDT respectively
          Primary Target K<sub>i</sub>4.4 nM for BRD4
          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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          Toxicity Standard Handling
          Storage -20°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

          BET Inhibitor, I-BET726 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Gosmini, R., et al. 2014. J. Med. Chem. 57, 811.
          Wyce, A., et al. 2013. Plos One. 8, e72967.
          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.

          Revision20-November-2015 JSW
          SynonymsBET Inhibitor, BET726, GSK1324726A, 4-((2S,4R)-1-Acetyl-4-((4-chlorophenyl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzoic acid
          DescriptionA cell-permeable tetrahydroquinoline based compound that acts as a highly potent and selective inhibitor of bromodomain and extra-terminal (BET) family proteins (IC50 = 41, 31, and 22 nM for BRD2, BRD3, BRD4, respectively). Binds to the acetyl-lysine recognition pocket of BET proteins and competes with tetra-acetylated histone H4 peptides (K5ac, K8ac, K12ac, K16ac) for binding to the bromodomains of these proteins. Does not affect the activity of over 50 different receptors, ion channels, and transporters even at higher concentrations (1-10 µM). Exhibits cytotoxicity towards neuroblastoma cell lines, induces apoptosis, and inhibits their growth (gIC50 = 26 and 60 nM for CHP-212 and SK-N-AS cells, respectively). Suppresses the growth of human neuroblastoma xenografts in murine models (5 mg/kg, p.o. for 2 weeks) and reduces the expression of MYCN and BCL2. Shown to improve survival rate of Balb/c mice subjected to LPS-induced (15 - 20 mg/kg) septic shock (10 mg/kg, i.v.). Displays desirable pharmacokinetic properties (t1/2 = 3.6 h; AUC 0-t = 6.03 µg/h/ml at 10 mg/kg i.v. in mice).
          FormLight yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₅H₂₃ClN₂O₃
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°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
          ReferencesGosmini, R., et al. 2014. J. Med. Chem. 57, 811.
          Wyce, A., et al. 2013. Plos One. 8, e72967.