GLPBio

UNC1215

Catalog No.: GC16794Purity:>98.00%Synonyms: UNC 1215;UNC-1215
Potent L3MBTL3 domain inhibitor

Products are for research use only. Not for human use. We do not sell to patients.


UNC1215
Cas No.: 1415800-43-9
10mM (in 1mL DMSO)In Stock
$63.00
1
1mgIn Stock
$27.00
1
5mgIn Stock
$54.00
1
10mgIn Stock
$90.00
1
50mgIn Stock
$342.00
1

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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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Description

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].
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.

Protocol

Cell experiment [1]:

Cell lines

Human embryonic kidney 293 cells transfected with a GFP fusion protein of the three MBT domains of L3MBTL3 (GFP-3MBT)

Preparation method

The solubility of this compound in DMSO is >26.05 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

EC50: 50–100 nM

Applications

Treatment with UNC1215 decreased the recovery time fluorescence intensity following photobleaching in a dose-responsive manner, with the EC50 of 50–100 nM, indicating that UNC1215 promoted diffusibility of GFP-3MBT within the nucleus. UNC1215 competed with cellular factors for binding of the MBT domains at concentrations well below 1 μM. UNC1215 showed potent effects on the subnuclear localization of GFP-3MBT, with an IC50 of approximately 500 nM for disruption of foci formation.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. James L I, Barsyte-Lovejoy D, Zhong N, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain[J]. Nature chemical biology, 2013, 9(3): 184-191.

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

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
SMILES
C1CCN(C1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)C(=O)N4CCC(CC4)N5CCCC5)NC6=CC=CC=C6
Molecular Formula
C32H43N5O2
Molecular Weight
529.72
Solubility
≥ 26.05 mg/mL in DMSO, ≥ 4.94 mg/mL in EtOH with ultrasonic and warming
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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