442640 | L3MBTL1 Ligand, UNC669 - Calbiochem

442640
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₂₀BrN₃O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      442640-25MG
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          Glass bottle 25 mg
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          Description
          OverviewA nicotinamido-pyrrolidine compound that targets the second MBT (Malignant Brain Tumor) module of "chromatin lock" L3MBTL1 (Lethal 3 MBT-Like protein 1; Kd = 5 µM by Isothermal titration calorimetry) that "reads"/binds mono- and dimethyl-lysine modified histones as well as other proteins involved in transcription, such as p53 and Rb, via methylation-dependent recognition. Shown to effectively compete against FAM-labeled, monomethylated Histone H3 (1-15) peptide (H3K9Me1) binding to L3MBTL1 (Kd = 10 µM in a FP displacement assay) and exhibit higher affinity toward L3MBTL1 than L3MBTL3 and L3MBTL4 (IC50 = 6, 35, and 69 µM, respectively, in a luminescent peptide competitive binding assay), while displaying no detectable binding toward four other methyl-lysine-binding proteins, the BMT domain-containing SFMBT1 and MBTD1, the PHD (Plant Homeodomain) finger-containing PHF13 (PHD finger 13), and the chromo domain-containing CBX7 (chromobox 7). As of end of 2012, no published data is available regarding the molecule's permeability or biological activity in cells.
          Catalogue Number442640
          Brand Family Calbiochem®
          Synonyms5-Bromo-N-(4-(pyrrolidinyl)piperidinyl)nicotinamide
          References
          ReferencesHerold, J.M., et al. 2011. J. Med. Chem. 54, 2504.
          Product Information
          FormPale orange-yellow solid
          Hill FormulaC₁₅H₂₀BrN₃O
          Chemical formulaC₁₅H₂₀BrN₃O
          Hygroscopic Hygroscopic
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥95% by HPLC
          Physicochemical Information
          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
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions 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) 

          Certificates of Analysis

          TitleLot Number
          442640

          References

          Reference overview
          Herold, J.M., et al. 2011. J. Med. Chem. 54, 2504.
          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.

          Revision02-April-2012 JSW
          Synonyms5-Bromo-N-(4-(pyrrolidinyl)piperidinyl)nicotinamide
          DescriptionA nicotinamido-pyrrolidine compound that targets the second MBT (Malignant Brain Tumor) module of "chromatin lock" L3MBTL1 (Lethal 3 MBT-Like protein 1; Kd = 5 µM by Isothermal titration calorimetry) that "reads"/binds mono- and dimethyl-lysine modified histones as well as other proteins involved in transcription, such as p53 and Rb, via methylation-dependent recognition. Shown to effectively compete against FAM-labeled, monomethylated Histone H3 (1-15) peptide (H3K9Me1) binding to L3MBTL1 (Kd = 10 µM in a FP displacement assay) and exhibit higher affinity toward L3MBTL1 than L3MBTL3 and L3MBTL4 (IC50 = 6, 35, and 69 µM, respectively, in a luminescent peptide competitive binding assay), while displaying no detectable binding toward four other methyl-lysine-binding proteins, the BMT domain-containing SFMBT1 and MBTD1, the PHD (Plant Homeodomain) finger-containing PHF13 (PHD finger 13), and the chromo domain-containing CBX7 (chromobox 7). As of end of 2012, no published data is available regarding the molecule's permeability or biological activity in cells.
          FormPale orange-yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₅H₂₀BrN₃O
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (50 mg/ml) or H₂O (2.5 mg/ml)
          Storage -20°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesHerold, J.M., et al. 2011. J. Med. Chem. 54, 2504.