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UNC1215

(CAS No:1415800-43-9)

UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family.

CAS No:1415800-43-9

Molecular Weight(MW):529.72

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	1415800-43-9
Molecular formula(MF)	C₃₂H₄₃N₅O₂
Molecular Weight(MW):	529.72
Alias

Solubility

In vitro	DMSO	100 mg/mL (188.77 mM)
	Ethanol	100 mg/mL (188.77 mM)
	Water	<1 mg/mL
In vivo

Biological Activity

Description

UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and K_d of 120 nM, 50-fold selective versus other members of the human MBT family.

Features

The first chemical probe for a Kme-binding protein.

Targets

L3MBTL3 ^[1]	L3MBTL3 ^[1]	L3MBTL3- D274A ^[1]
40 nM	120 nM(Kd)	3.5 μM

In vitro

UNC1215 binds L3MBTL3, competitively displacing mono- or dimethyllysine-containing peptides. This probe is greater than 50-fold selective versus other members of the human MBT family. UNC1215 has about a 75-fold selectivity for L3MBTL3 over L3MBTL1. UNC1215 shows no activity at concentrations up to 30 μM against the tandem Tudor domain of UHRF1, the chromodomain of CBX7 or the PHD domain of JARID1A. X-ray crystallography identifies 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. UNC1215 is used to reveal a new Kme-dependent interaction of L3MBTL3 with BCLAF1, a protein implicated in DNA damage repair and apoptosis. ^[1]