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说明： Antagonizes PWWP1 interaction with nucleosomal H3K36me2, alters NSD2 nucleolar localization
化学名： N-Cyclopropyl-3,4-dihydro-3-oxo-N-[[4-[(4-pyrimidinylamino)carbonyl]phenyl]methyl]-2H-1,4-benzoxazine-7-carboxamide
纯度： ≥98% (HPLC)
生物活性 for UNC 6934
UNC 6934 binds to the N-terminal proline-tryptophan-tryptophan-proline (PWWP) domain of nuclear receptor-binding SET domain-containing 2 (NSD2). UNC 6934 inhibits PWWP1 interaction with nucleosomal H3K36me2 (IC50 = 104 nM) by occupying the canonical H3K36me2-binding pocket of PWWP1. It selectively binds endogenous NSD2 in cells and causes accumulation of endogenous NSD2 in the nucleolus.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 6934 probe summary on the SGC website.
技术数据 for UNC 6934
| 分子量 | 443.46 |
| 公式 | C24H21N5O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2561494-77-5 |
| PubChem ID | 146676966 |
| InChI Key | KOZGEDUWAQFVAV-UHFFFAOYSA-N |
| Smiles | O=C(C1=CC=C(N2)C(OCC2=O)=C1)N(C3CC3)CC4=CC=C(C(NC5=NC=NC=C5)=O)C=C4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for UNC 6934
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 8.87 | 20 |
制备储备液 for UNC 6934
以下数据基于产品分子量 443.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 11.27 mL | 56.37 mL | 112.75 mL |
| 1 mM | 2.25 mL | 11.27 mL | 22.55 mL |
| 2 mM | 1.13 mL | 5.64 mL | 11.27 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.25 mL |
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产品说明书 for UNC 6934
参考文献 for UNC 6934
参考文献是支持产品生物活性的出版物。
Dilworth et al (2022) A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization. Nat.Chem.Biol. 18 56 PMID: 34782742
Sankaran et al (2016) A PWWP domain of histone-lysine N-methyltransferase NSD2 binds to dimethylated Lys-36 of histone H3 and regulates NSD2 function at chromatin. J.Biol.Chem. 291 8465 PMID: 26912663
If you know of a relevant reference for UNC 6934, please let us know.
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关键词: UNC 6934, UNC 6934 supplier, UNC6934, antagonists, antagonizing, methyltransferase, NSD2, PWWP, H3K36me2, interaction, Other, Lysine, Methyltransferases, 7183, Tocris Bioscience
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