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442640 L3MBTL1 Ligand, UNC669 - Calbiochem

442640
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₅H₂₀BrN₃O

Products

Catalogue NumberPackaging Qty/Pack
442640-25MG Glass bottle 25 mg
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
Quality LevelMQ100
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

L3MBTL1 Ligand, UNC669 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

L3MBTL1 Ligand, UNC669 - Calbiochem 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.