442640-M

L3MBTL1 Ligand, UNC669

A nicotinamido-pyrrolidine compound that targets the second MBT (Malignant Brain Tumor) module of "chromatin lock" L3MBTL1.

• Synonym(s): L3MBTL1 Ligand, UNC669, 5-Bromo-N-(4-(pyrrolidinyl)piperidinyl)nicotinamide
• Empirical Formula (Hill Notation): C₁₅H₂₀BrN₃O
• Molecular Weight: 338.24
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: pale orange-yellow
• solubility: water: 2.5 mg/mL; DMSO: 50 mg/mL
• storage temp.: −20°C

Description

General description

A nicotinamido-pyrrolidine compound that targets the second MBT (Malignant Brain Tumor) module of "chromatin lock" L3MBTL1 (Lethal 3 MBT-Like protein 1; K_d = 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 (K_d = 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.

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable