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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-UNC6934
UNC6934

Chemical Structure : UNC6934

CAS No.: 2561494-77-5

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UNC6934 (UNC-6934)

货号: PC-49209Not For Human Use, Lab Use Only.

UNC6934 is a potent, selective chemical probe ligand targeting the N-terminal PWWP (PWWP1) domain of NSD2 with Kd value of 91 nM, selectively binds in the aromatic cage of NSD2-PWWP1, thereby disrupting its interaction with H3K36me2 nucleosomes.

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5 mg ￥1980 In stock
10 mg ￥2980 In stock
25 mg ￥4880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

UNC6934 is a potent, selective chemical probe ligand targeting the N-terminal PWWP (PWWP1) domain of NSD2 with Kd value of 91 nM, selectively binds in the aromatic cage of NSD2-PWWP1, thereby disrupting its interaction with H3K36me2 nucleosomes.
UNC6934 occupies the canonical H3K36me2-binding pocket of PWWP1, antagonizes PWWP1 interaction with nucleosomal H3K36me2 and selectively engages endogenous NSD2 in cells.
UNC6934 induces accumulation of endogenous NSD2 in the nucleolus, phenocopying the localization defects of NSD2 protein isoforms lacking PWWP1 that result from translocations prevalent in multiple myeloma (MM).
UNC6934 is selective for NSD2-PWWP1 over 14 other human PWWP domains and does not inhibit any of a panel of 33 methyltransferase domains including the H3K36 methyltransferases, NSD1, NSD2, NSD3, and SETD2.
UNC6934 selectively engages NSD2 in live cells (U2OS cell) with EC50 of 1.23 uM.
UNC6934 promotes enrichment of endogenous NSD2 in the nucleolus.

物理化学性质&存储条件

分子量 443.463
分子式 C24H21N5O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-cyclopropyl-3-oxo-N-(4-(pyrimidin-4-ylcarbamoyl)benzyl)-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide

参考文献

1. David Dilworth, et al. Nat Chem Biol. 2022 Jan;18(1):56-63.

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