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NR 162

Cat. No. 7572 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 calcium/calmodulin-dependent serine protein kinase (CASK) inhibitor
化学名： 4-(Cyclopentylamino)-2-((2,5-dibromo-4-methylbenzyl)amino)-N-(3-(2-oxooxazolidin-3-yl)propyl)pyrimidine-5-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
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 NR 162

NR 162 is a potent and selective calcium/calmodulin-dependent serine protein kinase (CASK) inhibitor (IC50 = 80 nM); it exhibits no significant activity against related kinases MERTK, AXL and ABL1 and ~ 47-fold selectivity over TYRO3 (IC50 = 3.8 μM). NR 162 targets the unique pocket created by CASK GFG motif; it is a type-I inhibitor which stabilizes the active state of CASK without affecting the scaffolding function. NR 162 induces cell death in actively differentiating cells of the P19 neuronal differentiation model. NR 162 shows no toxicity in differentiated cells, or in cancer cells.

许可信息

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the NR 162 probe summary on the SGC website.

技术数据 for NR 162

分子量 610.35
公式 C24H30Br2N6O3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2755241-73-5
PubChem ID 155908701
InChI Key BPLPIBNWDLPUKP-UHFFFAOYSA-N
Smiles O=C(C1=CN=C(N=C1NC2CCCC2)NCC3=CC(Br)=C(C=C3Br)C)NCCCN4CCOC4=O

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 NR 162

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 12.21 20
ethanol 3.05 5

制备储备液 for NR 162

以下数据基于产品分子量 610.35。 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
0.2 mM 8.19 mL 40.96 mL 81.92 mL
1 mM 1.64 mL 8.19 mL 16.38 mL
2 mM 0.82 mL 4.1 mL 8.19 mL
10 mM 0.16 mL 0.82 mL 1.64 mL

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参考文献 for NR 162

参考文献是支持产品生物活性的出版物。

Russ et al (2021) Design and development of a chemical probe for pseudokinase Ca2+/calmodulin-dependent Ser/Thr kinase. J.Med.Chem. 64 14358 PMID: 34543009

If you know of a relevant reference for NR 162, please let us know.

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关键词: NR 162, NR 162 supplier, NR162, type-I, inhibitor, inhibits, potent, selective, calcium/calmodulin-dependent, serine, protein, kinase, CASK, GFG, calmodulin, CaM, Kinase, 7572, Tocris Bioscience

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