UNC1215

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.

CAS No. 1415800-43-9

サイズ	価格(税別)	在庫状況
5mg	JPY 18100	国内在庫あり
25mg	JPY 63400	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（7）

製品安全説明書

現在のバッチを見る：純度： 99.73%

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UNC1215関連製品

関連ターゲット	BET p300/CBP BRPF bromodomain	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ	もっと見る

シグナル伝達経路

Epigenetic Reader Domainシグナル伝達経路

Epigenetic Reader Domain阻害剤の選択性比較

生物活性

製品説明

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.

特性

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
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]
Kinase Assay	AlphaScreen assay
Kinase Assay	Compound plates (1 μL at 10 or 30 mM highest concentration) are diluted in 1×assay buffer (20 mM Tris pH 8.0, 25 mM NaCl, 2 mM DTT and 0.05% Tween-20) over 2 steps using a Multimek robotic pipettor and 1 μL is spotted into the wells of 384-well assay Proxiplates. To these plates 9 μL of protein- peptide mix in 1× assay buffer is added by Multidrop and incubated for 30 min at room temperature. At this point 2 μL of streptavidin-conjugate donor and nickel-chelate acceptor beads (45 μg/mL in 1× assay buffer) are added, the plates are allowed to incubate for an additional 30 min in the dark at room temperature. After incubation the plates are read on EnVision mulilabel reader equipped with HTS alpha screen laser. The screens reported are performed up to 10 or 30 μM, and therefore it should be noted that those compounds referred to as inactive are indeed inactive only within the concentration range tested. PHF23 and JARID1A are GST tagged and consequently for these assays GST-acceptor beads are used. It should be noted that any positive binding curves for L3MBTL4 that are generated yielded curves with very shallow slopes, suggesting a nonspecific interaction. The data for the IC50 values is calculated from replicate runs in that the datapoints for each compound concentration are averaged and plotted using 4-parameters curve fitting.
細胞実験	細胞株	HEK293T/17 cells
	濃度	~100 μM
	反応時間	24 h
	実験の流れ	CellTiter-Glo luminescent cell viability assay

参考
[1] James LI, et al. Nat Chem Biol, 2013, 9(3), 184-191.

参考

[1] James LI, et al. Nat Chem Biol, 2013, 9(3), 184-191.

化学情報

分子量	529.72	化学式	C₃₂H₄₃N₅O₂
CAS No.	1415800-43-9	SDF	Download UNC1215 SDFをダウンロードする
Smiles	C1CCN(C1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)C(=O)N4CCC(CC4)N5CCCC5)NC6=CC=CC=C6
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (188.77 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):