UNC1215

- Overview
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    Background
    
    UNC1215 is a selective inhibitor of L3MBTL3 with IC50 value of 40 nM [1].L3MBTL3 is a member of the MBT (malignant brain tumor) family of methyl-lysine reader proteins and is reported to play an important role in haematopoiesis and cancer biology. And it is reported that inhibition of L3MBTL3 can be regarded as a promising target used in clinic [2]. UNC1215 is a potent L3MBTL3 inhibitor and has a more potent inhibitory ability than other MBT family members. When tested with HEK293 cells transfected with a GFP fusion protein of the 3 MBT domains of L3MBTL3, UNC1215 treatment decreased the recovery time in a dose responsive manner via binding and co-localizing L3MBTL3 [1]. Using AlphaScreen○R methylated histone peptide competition assay, UNC1215 showed high antagonism ability to L3MBTL3 with IC50 value of 24±7.6 nM [3]. As the first potent and selective inhibitor for methyl-lysine reader protein-L3MBTL3-UNC1215 showed highly selective inhibitor ability via antagonizing the mono- and dimethyl-lysine reading function of L3MBTL3 [2].
    
    1. James, L.I., et al., Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol, 2013. 9(3): p. 184-91.
    2. James, L.I., et al., Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem, 2013. 56(18): p. 7358-71.
    3. Camerino, M.A., et al., The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface. Medchemcomm, 2013. 4(11): p. 1501-1507.
- Properties
  - Categories
    
    Chemical probe for the methyllysine (Kme)
    
    Alternative Name
    
    UNC 1215;UNC-1215; [3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone
    
    CAS Number
    
    1415800-43-9
    
    Molecular Formula
    
    C32H43N5O2
    
    Molecular Weight
    
    529.72
    
    Appearance
    
    A solid
    
    Purity
    
    98.55%
    
    Solubility
    
    ≥26.05 mg/mL in DMSO; insoluble in H2O; ≥4.94 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    C1CCN(C1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)C(=O)N4CCC(CC4)N5CCCC5)NC6=CC=CC=C6
    
    * For Research Use Only
- Reference
  - 1. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031

Documents

COA (Certificate Of Analysis)

HPLC (Retest)

NMR (Nuclear Magnetic Resonance)

MSDS (Material Safety Data Sheet)

Datasheet

UNC1215

Background

Documents

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