UNC1215

製品コードS7088 バッチS708802

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C32H43N5O2
分子量 529.72 CAS No. 1415800-43-9
Solubility (25°C)* 体外 DMSO 100 mg/mL (188.77 mM)
Ethanol 100 mg/mL (188.77 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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 Kd of 120 nM, 50-fold selective versus other members of the human MBT family.
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]
特徴 The first chemical probe for a Kme-binding protein.

プロトコル(参考用のみ)

キナーゼアッセイ AlphaScreen 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.
細胞アッセイ 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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Recapitulating early human development with 8C-like cells [ Cell Rep, 2022, 39(12):110994] PubMed: 35732112
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Peroxisome-driven ether-linked phospholipids biosynthesis is essential for ferroptosis [ Cell Death Differ, 2021, 10.1038/s41418-021-00769-0] PubMed: 33731874
Prolonged unfolded protein reaction is involved in the induction of chronic myeloid leukemia cell death upon oprozomib treatment [ Cancer Sci, 2020, 112(1):133-143] PubMed: 33067904
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193
[ Cell Death Dis, 2018, ] PubMed: 29988031
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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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