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MLN 4924

Cat. No. 6499 1 次引用 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective NEDD8 activating enzyme (NAE) inhibitor; cell permeable
别名： Pevonedistat,TAK-924
化学名： [(1S,2S,4R)-4-[4-[[(1S)-2,3-Dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl sulfamic acid ester
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for MLN 4924

MLN 4924 (TAK 924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50 = 4.7 nM). MLN 4924 exhibits selectivity over closely related enzymes UAE, UBA6, SAE, and ATG7 (IC50 = 1.5, 1.8, 8.2, and >10 μM, respectively), and displays minimal activity at adenosine receptors and a panel of 12 cellular kinases. MLN 4924 exhibits cyotoxicity in several human tumor-derived cell lines and causes liver damage in SD rats, when given with TNF-α. It blocks the NEDD8 pathway causing DNA damage in mice bearing HCT-116 xenografts. Cell permeable.

技术数据 for MLN 4924

分子量 443.52
公式 C21H25N5O4S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 905579-51-3
PubChem ID 16720766
InChI Key MPUQHZXIXSTTDU-QXGSTGNESA-N
Smiles N[S](=O)(=O)OC[C@@H]1C[C@H](C[C@@H]1O)N1C=CC2=C(N[C@H]3CCC4=CC=CC=C34)N=CN=C12

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 MLN 4924

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 44.35 100
ethanol 44.35 100

制备储备液 for MLN 4924

以下数据基于产品分子量 443.52。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.25 mL 11.27 mL 22.55 mL
5 mM 0.45 mL 2.25 mL 4.51 mL
10 mM 0.23 mL 1.13 mL 2.25 mL
50 mM 0.05 mL 0.23 mL 0.45 mL

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产品说明书 for MLN 4924

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for MLN 4924

参考文献是支持产品生物活性的出版物。

Baek et al (2020) NEDD8 nucleates a multivalent cullin-RING-UBE2D ubiquitin ligation assembly. Nature 578 461 PMID: 32051583

Soucy et al (2009) An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 458 732 PMID: 19360080

Brownell et al (2010) Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ. Mol.Cell 37 102 PMID: 20129059

Zhou et al (2016) Blockage of neddylation modification stimulates tumor sphere formation in vitro and stem cell differentiation and wound healing in vivo. Proc.Natl.Acad.Sci.USA 113 E2935 PMID: 27162365

Hyer et al (2018) A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat.Med. 24 186 PMID: 29334375

Tong et al (2017) MLN4924 (Pevonedistat), a protein neddylation inhibitor, suppresses proliferation and migration of human clear cell renal cell carcinoma. Sci.Rep. 7 5599 PMID: 28717191

Wolenski et al (2015) The NAE inhibitor pevonedistat (MLN4924) synergizes with TNF-α to activate apoptosis. Cell Death Discov. 1 doi: 10.1038 PMID: 27551465

If you know of a relevant reference for MLN 4924, please let us know.

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关键词: MLN 4924, MLN 4924 supplier, MLN4924, NEDD8, activating, enzymes, NAE, inhibitor, inhibitors, inhibits, neddylation, cell, permeable, Pevonedistat, TAK-924, Other, Ligases, 6499, Tocris Bioscience

1 篇 MLN 4924 的引用文献

引用文献是使用了 Tocris 产品的出版物。 MLN 4924 的部分引用包括：

Bruno et al (2022) Human NLRP1 is a sensor of pathogenic coronavirus 3CL proteases in lung epithelial cells. Mol Cell 82 2385-2400.e9 PMID: 35594856

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