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Submit ReviewCRT 0066101
说明： Potent protein kinase D (PKD) inhibitor
化学名： 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride
纯度： ≥98% (HPLC)
生物活性 for CRT 0066101
CRT 0066101 is a potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC50 values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively). Exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, MEK, ERK, c-Raf and c-Src. Reduces proliferation and cell viability of pancreatic cancer cells expressing moderate levels of endogenous PKD1/2. Orally bioavailable.
技术数据 for CRT 0066101
| 分子量 | 411.33 |
| 公式 | C18H22N6O.2HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1883545-60-5 |
| PubChem ID | 69074905 |
| InChI Key | CXYCRYGNFKDPRH-FMOMHUKBSA-N |
| Smiles | OC1=C(C3=NC(NC[C@@H](CC)N)=CC=N3)C=C(C2=CN(C)N=C2)C=C1.Cl.Cl |
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 CRT 0066101
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 41.13 | 100 | |
| DMSO | 8.23 | 20 |
制备储备液 for CRT 0066101
以下数据基于产品分子量 411.33。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.43 mL | 12.16 mL | 24.31 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.86 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.43 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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产品说明书 for CRT 0066101
参考文献 for CRT 0066101
参考文献是支持产品生物活性的出版物。
Harikumar et al (2010) A novel small molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo. Mol.Cancer Ther. 9 1136 PMID: 20442301
Ni et al (2013) PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS ONE 9 e73149 PMID: 24039875
If you know of a relevant reference for CRT 0066101, please let us know.
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关键词: CRT 0066101, CRT 0066101 supplier, CRT0066101, potent, pan, protein, kinase, D, PKD, PKD1, PKD2, PKD3, inhibits, inhibitors, Protein, Kinase, 4975, Tocris Bioscience
7 篇 CRT 0066101 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CRT 0066101 的部分引用包括：
Zhang et al (2017) Protein kinase D at the Golgi controls NLRP3 inflammasome activation. J Exp Med 214 2671 PMID: 28716882
Liou et al (2015) Protein kinase D1 drives pancreatic acinar cell reprogramming and progression to intraepithelial neoplasia. Sci Rep 6 6200 PMID: 25698580
Steve N et al (2021) Inhibiting Protein Kinase D Promotes Airway Epithelial Barrier Integrity in Mouse Models of Influenza A Virus Infection. Front Immunol 11 580401 PMID: 33381112
Ben et al (2021) Evaluation of protein kinase D auto-phosphorylation as biomarker for NLRP3 inflammasome activation. PLoS One 16 e0248668 PMID: 34767572
Stephan A et al (2021) Protein kinase D promotes activity-dependent AMPA receptor endocytosis in hippocampal neurons. Traffic 22 454-470 PMID: 34564930
Jensen et al (2016) Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the Golgi apparatus to the plasma membrane. J.Biol.Chem. 291 11285 PMID: 27030010
Peter et al (2020) The GEF-H1/PKD3 signaling pathway promotes the maintenance of triple-negative breast cancer stem cells. Int J Cancer 146 3423-3434 PMID: 31745977
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CRT 0066101 的评论
平均评分: 5 (基于 4 条评论。)
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Good and reliable PKD inhibitor.
By
Anonymous on 09/20/2019
分析类型： In Vivo
种属： Mouse
Used in an in-vivo behavioral assay
Easy to dissolve in solution, works great in an in-vivo animal study. (Mechanical allodynia assay). Good and reliable PKD inhibitor
Lysophospatidic acid promotes microglia motility via the LPAR5-PKD axis..
By
lisha joshi on 06/10/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： BV2 microglia cells
The inhibitor was dissolved in DMSO and used at a concentration of 1µM (concentrations of 0.1µM and 0.5µM were also tested but we observed more potent inhibition with 1µM). BV2 microglia were treated with LPA (1µM) in the presence or absence of CRT. Using a time lapse microscope we analyzed the impact of PKD family inhibition on the LPA induced microglial migration.
PKD family inhibition in LPA induced pro-inflammatory phenotype in microglia.
By
Joanna Plastira on 06/08/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： Primary murine microglia cells
Primary murine microglia were incubated for different time points with LPA (1µM) in the presence or absence of CRT (1µM). CRT significantly inhibited the expression of COX2 and promoted the expression of Arg1. DMSO can sometimes induce an expression (for different proteins) under control conditions. We observed this problem in BV2 cell line (but not in primary cells). In this case it is best to dilute the CRT in water.
Very potent PKD inhibitor.
By
Anonymous on 11/06/2017
分析类型： In Vivo
种属： Mouse
The product was used per os on mice for an invivo study.
the CRT0066101 PKD inhibitor can be dissolved in normal saline or DMSO easily (depends of the concentration)