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UNC1215 1415800-43-9
UNC1215 is a selective inhibitor of L3MBTL3 with IC50 value of 40 nM [1].
| Cas No. | 1415800-43-9 |
| Synonyms | UNC 1215;UNC-1215 |
| Chemical Name | [3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone |
| Canonical SMILES | C1CCN(C1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)C(=O)N4CCC(CC4)N5CCCC5)NC6=CC=CC=C6 |
| Formula | C32H43N5O2 |
| M.Wt | 529.72 |
| Storage | Store at -20°C |
| Solubility | ≥ 26.05 mg/mL in DMSO, ≥ 4.94 mg/mL in EtOH with ultrasonic and warming |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. |
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
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].
References:
[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.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.