500557 | L3MBTL3 MBT Domain Blocker, UNC1215 - Calbiochem

500557
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₂H₄₃N₅O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00557.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable pyrrolidinyl-piperidinyl-benzamide that effectively competes against H4K20Me2 peptide for L3MBTL3 binding by targeting the first two L3MBTL3 MBT domains (Kd = 120 nM in binding studies using recombinant 3MBT fragment), while exhibiting much reduced potency against L3MBTL1-H4K20Me1, 53BP1-H4K20Me2, MBTD1-H4K20Me1, or L3MBTL4-H2AK36Me1 interaction (IC50 ≥2 µM; [peptide] = 150 nM). Shown to increase GFP-L3MBTL fusion nucleus mobility (10 nM to 1 µM) in HEK293 transfectants. X-ray structural analysis reveals two 3MBT are bridged together by two UNC1215 molecules in a reciprocal fashion.

          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 Number500557
          Brand Family Calbiochem®
          Synonyms2-Phenylamino-1,4-bis(4-(pyrrolidinyl)piperidinyl)benzamide, TFA, 2-(Phenylamino)-1,4-phenylene-bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone, TFA, Lethal(3)malignant Brain Tumor-Like Protein 3 MBT Domain Blocker
          References
          ReferencesJames, L.I., et al. 2013. Nat. Chem. Biol. 9, 184.
          Product Information
          FormOff-white powder
          Hill FormulaC₃₂H₄₃N₅O₂
          Chemical formulaC₃₂H₄₃N₅O₂
          Hygroscopic Hygroscopic
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetKme binding ligand of L3MBTL3
          Primary Target IC<sub>50</sub>40 nM)
          Primary Target K<sub>i</sub>0.12 µ
          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 Ambient Temperature Only
          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 3 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
          James, L.I., et al. 2013. Nat. Chem. Biol. 9, 184.
          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.

          Revision17-May-2013 JSW
          Synonyms2-Phenylamino-1,4-bis(4-(pyrrolidinyl)piperidinyl)benzamide, TFA, 2-(Phenylamino)-1,4-phenylene-bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone, TFA, Lethal(3)malignant Brain Tumor-Like Protein 3 MBT Domain Blocker
          DescriptionA cell-permeable, highly stable (no degradation in 72 h in HEK cultures), non-cytotoxic (up to 100 µM and 24 h in HEK293T/17 cultures) pyrrolidinyl-piperidinyl-benzamide compound that effectively competes against H4K20me2 peptide (aa 17-25; 150 nM) for L3MBTL3 (200 nM) binding (IC50 = 40 nM) by targeting the first two L3MBTL3 MBT domains (Kd = 120 nM in binding studies using recombinant 3MBT fragment), while exhibiting much reduced potency against L3MBTL1-H4K20me, 53BP1-H4K20me2, MBTD1-H4K20me, or L3MBTL4-H2AK36me interaction (IC50 = 2, 4, 11, and 16 µM, respectively; [peptide] = 150 nM). Selectivity profiling against panels of non-Kme readers likewise reveals only weak UNC1215 potency against FLT3 kinase activity (by 64% at 10 µM), M1-mediated Ca2+ mobilization (IC50 = 3.6 µM; stimulant = 10 nM acetylcholine), or M2-mediated cAMP production (by 30% at 30 µM; stimulant = 100 nM acetylcholine). UNC1215 is shown to increase GFP-full-length L3MBTL fusion (GFP-FLMBT) nucleus mobility in a dose-dependent manner (10 nM to 1 µM; by FRAP) and fluorescent mero76-UNC1215 conjugate is demonstrated to co-localize with GFP-FLMBT in HEK293 transfectants. X-ray structural analysis using 3MBT fragment reveals two 3MBT are bridged together by two UNC1215 molecules in a reciprocal fashion, with the domain 1 and 2 Kme-binding pocket of each 3MBT being targeted by a different UNC1215 molecule and with each UNC1215 simultaneously targeting domain 1 from one 3MBT and domain 2 from the other 3MBT.
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₃₂H₄₃N₅O₂
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (10 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesJames, L.I., et al. 2013. Nat. Chem. Biol. 9, 184.