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Description: Antagonizes PWWP1 interaction with nucleosomal H3K36me2, alters NSD2 nucleolar localization
Chemical Name: N-Cyclopropyl-3,4-dihydro-3-oxo-N-[[4-[(4-pyrimidinylamino)carbonyl]phenyl]methyl]-2H-1,4-benzoxazine-7-carboxamide
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
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.
Technical Data for UNC 6934
| M. Wt | 443.46 |
| Formula | C24H21N5O4 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for UNC 6934
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.87 | 20 |
Preparing Stock Solutions for UNC 6934
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for UNC 6934
References for UNC 6934
References are publications that support the biological activity of the product.
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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Keywords: UNC 6934, UNC 6934 supplier, UNC6934, antagonists, antagonizing, methyltransferase, NSD2, PWWP, H3K36me2, interaction, Other, Lysine, Methyltransferases, 7183, Tocris Bioscience
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