NCC007
目录号 : GC36708
NCC007 是一种双酪蛋白激酶 Iα (CKIα) 和 δ (CKIδ) 抑制剂，IC50 分别为 1.8 和 3.6 μM。NCC007 可用于哺乳动物昼夜节律的研究。
Cas No.:2342583-66-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms[1]. CKIα|1.8 μM (IC50)|CKIδ|3.6 μM (IC50)
NCC007 (5-15 mM, infused into the lateral ventricle) controls circadian rhythms through CKI inhibition[1]. Animal Model: Adult C57BL/6J background male mice (8 weeks old)[1]
[1]. Lee JW, et al. Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ. J Med Chem. 2019 Feb 28;62(4):1989-1998.
| Cas No. | 2342583-66-6 | SDF | |
| Canonical SMILES | CN(C)CCNC1=NC2=C(N=CN2C(C)C3CC3)C(NCC4=CC(C(F)(F)F)=CC=C4)=N1 | ||
| 分子式 | C22H28F3N7 | 分子量 | 447.5 |
| 溶解度 | DMSO: 125 mg/mL (279.33 mM) | 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 | 2.2346 mL | 11.1732 mL | 22.3464 mL |
| 5 mM | 0.4469 mL | 2.2346 mL | 4.4693 mL |
| 10 mM | 0.2235 mL | 1.1173 mL | 2.2346 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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。
Chemical Control of Mammalian Circadian Behavior through Dual Inhibition of Casein Kinase Iα and δ
J Med Chem 2019 Feb 28;62(4):1989-1998.PMID:30707835DOI:PMC8901179
Circadian rhythms are controlled by transcriptional feedback loops of clock genes and proteins. The stability of clock proteins is regulated by post-translational modification, such as phosphorylation by kinases. In particular, casein kinase I (CKI) phosphorylates the PER protein to regulate proteasomal degradation and nuclear localization. Therefore, CKI inhibition can modulate mammalian circadian rhythms. In the present study, we have developed novel CKIα and CKIδ dual inhibitors by extensive structural modification of N9 and C2 position of longdaysin. We identified NCC007 that showed stronger period effects (0.32 μM for 5 h period lengthening) in a cell-based circadian assay. The following in vitro kinase assay showed that NCC007 inhibited CKIα and CKIδ with an IC50 of 1.8 and 3.6 μM. We further demonstrated that NCC007 lengthened the period of mouse behavioral rhythms in vivo. Thus, NCC007 is a valuable tool compound to control circadian rhythms through CKI inhibition.