UNC1215

Names

[ Name ]:
UNC1215

[Synonym ]:
(2-Anilino-1,4-phenylene)bis{[4-(1-pyrrolidinyl)-1-piperidinyl]methanone}
Methanone, 1,1'-[2-(phenylamino)-1,4-phenylene]bis[1-[4-(1-pyrrolidinyl)-1-piperidinyl]-

Biological Activity

[Description]:

UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.IC50 Value: 120 nM (Kd) [1]Target: L3MBTL3 In vitro: UNC1215 binds L3MBTL3 with a K(d) of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a unique 2:2 polyvalent mode of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization [1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

Research Areas >> Cancer

[References]

[1]. James LI, Barsyte-Lovejoy D, Zhong N, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol. 2013 Mar;9(3):184-91. doi: 10.1038/nchembio.1157.

[Related Small Molecules]

GSK126 | Tazemetostat (EPZ-6438) | UNC 0642 | GSK343 | Pinometostat (EPZ5676) | 3-Deazaneplanocin A (hydrochloride) | Pemrametostat (GSK3326595) | UNC1999 | BIX-01294 | EPZ031686 | AZ505 (ditrifluoroacetate) | MS023 | EPZ 004777 | EPZ015666 | EPZ015866(GSK591)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
712.1±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₂H₄₃N₅O₂

[ Molecular Weight ]:
529.716

[ Flash Point ]:
384.5±32.9 °C

[ Exact Mass ]:
529.341675

[ PSA ]:
59.13000

[ LogP ]:
3.37

[ Appearance of Characters ]:
white to beige

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.640

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: soluble5mg/mL, clear

Safety Information

[ RIDADR ]:
NONH for all modes of transport