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500557 L3MBTL3 MBT Domain Blocker, UNC1215 - Calbiochem

500557
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₃₂H₄₃N₅O₂

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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
      Quality LevelMQ100
      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

      L3MBTL3 MBT Domain Blocker, UNC1215 - Calbiochem 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.