533169 BET Inhibitor, I-BET726 - Calbiochem

533169
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₅H₂₃ClN₂O₃

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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
      Quality LevelMQ100
      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.