UNC6934
目录号 : GC64083
UNC6934 is a a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2. UNC6934 is a potent antagonist of NSD2-PWWP1 with a Kd (SPR) of 80 nM and is selective for NSD2-PWWP1 over 14 other PWWP domains including NSD3-PWWP1 UNC6934 disrupts the NSD2-PWWP1 interaction with H3K36me2 nucleosomes in U2OS cells as measured by a NanoBret assay with an IC50 of 1.09 μM.
Cas No.:2561494-77-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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- Datasheet
UNC6934 is a a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2. UNC6934 is a potent antagonist of NSD2-PWWP1 with a Kd (SPR) of 80 nM and is selective for NSD2-PWWP1 over 14 other PWWP domains including NSD3-PWWP1 UNC6934 disrupts the NSD2-PWWP1 interaction with H3K36me2 nucleosomes in U2OS cells as measured by a NanoBret assay with an IC50 of 1.09 μM.
UNC6934-mediated antagonism of PWWP1 leads to accumulation of endogenous NSD2 in the nucleolus. [1]
[1] Dilworth D, et al. Nat Chem Biol. 2022 Jan;18(1):56-63.
| Cas No. | 2561494-77-5 | SDF | Download SDF |
| 分子式 | C24H21N5O4 | 分子量 | 443.45 |
| 溶解度 | DMSO : 25 mg/mL (56.38 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.255 mL | 11.2752 mL | 22.5505 mL |
| 5 mM | 0.451 mL | 2.255 mL | 4.5101 mL |
| 10 mM | 0.2255 mL | 1.1275 mL | 2.255 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization
Nat Chem Biol 2022 Jan;18(1):56-63.PMID:34782742DOI:PMC9189931
Nuclear receptor-binding SET domain-containing 2 (NSD2) is the primary enzyme responsible for the dimethylation of lysine 36 of histone 3 (H3K36), a mark associated with active gene transcription and intergenic DNA methylation. In addition to a methyltransferase domain, NSD2 harbors two proline-tryptophan-tryptophan-proline (PWWP) domains and five plant homeodomains (PHDs) believed to serve as chromatin reading modules. Here, we report a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2. 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). Mutations of other NSD2 chromatin reader domains also increase NSD2 nucleolar localization and enhance the effect of UNC6934. This chemical probe and the accompanying negative control UNC7145 will be useful tools in defining NSD2 biology.