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Submit ReviewCalyculin A is a potent and selective cell-permeable inhibitor of protein phosphatase 1 (IC50 = 0.3 - 0.7 nM) and protein phosphatase 2A (IC50 = 0.5 - 1 nM). Displays > 10,000,000-fold selectivity over PP2B and PP2C.
Note: This product is typically prepared in DMSO.
分子量 | 1009.18 |
公式 | C50H81N4O15P |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 101932-71-2 |
PubChem ID | 3894 |
InChI Key | ULTTYPMRMMDONC-UHFFFAOYSA-N |
Smiles | O[C@H]1[C@H](C)[C@H](C/C=C/C3=COC([C@@H](C)CCNC([C@H]([C@H]([C@@H](N(C)C)COC)O)O)=O)=N3)O[C@]2([C@](C)(C)[C@@H](OP(O)(O)=O)[C@]([C@@H](OC)C[C@H](O)[C@H](C)[C@H](O)[C@H](C)/C=C(C)/C(C)=C/C=C/C(C)=C\C#N)([H])O2)C1 |
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.
参考文献是支持产品生物活性的出版物。
Favre et al (1997) Differential inhibition and posttranslational modification of protein phosphatase 1 and 2A in MCF7 cells treated with calyculin-A, okadaic acid, and tautomycin. J.Biol.Chem. 272 13856 PMID: 9153244
Ishihara et al (1989) Calyculin A and okadaic acid: inhibitors of protein phosphatase activity. Biochem.Biophys.Res.Commun. 159 871 PMID: 2539153
Lindval et al (1997) The binding mode of calyculin A to protein phosphatase-1. J.Biol.Chem. 272 23312 PMID: 9287341
McCluskey et al (2002) Serine-threonine protein phosphatase inhibitors: development of therapeutic strategies. J.Med.Chem. 45 1151 PMID: 11881984
If you know of a relevant reference for Calyculin A, please let us know.
关键词: Calyculin A, Calyculin A supplier, Protein, phosphatase, 1, 2A, inhibitors, inhibits, Calcineurin, Ser/Thr, Phosphatases, PP1, PP2A, CalyculinA, 1336, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Calyculin A 的部分引用包括:
Kii et al (2016) Selective inhibition of the kinase DYRK1A by targeting its folding process. Nat Commun 7 11391 PMID: 27102360
Burdyga et al (2018) Phosphatases control PKA-dependent functional microdomains at the outer mitochondrial membrane. Proc Natl Acad Sci U S A. 115 E6497 PMID: 29941564
Liu (2018) In vivo brain GPCR signaling elucidated by phosphoproteomics. Science 360 eaao4927 PMID: 29930108
Chazeau et al (2015) Mechanical coupling between transsynaptic N-cadherin adhesions and actin flow stabilizes dendritic spines. J Neurochem 26 859 PMID: 25568337
Bhattachariya et al (2014) PYK2 selectively mediates signals for growth versus differentiation in response to stretch of spontaneously active vascular smooth muscle. Physiol Rep 2 PMID: 25347863
Fabbrizi et al (2018) Transient PP2A inhibition alleviates normal tissue stem cell susceptibility to cell death during radiotherapy. Cell Death Dis 9 492 PMID: 29706648
Isensee et al (2014) Pain modulators regulate the dynamics of PKA-RII phosphorylation in subgroups of sensory neurons. J Cell Sci 127 216 PMID: 24190886
Chiu et al (2019) NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content. Cell Rep 28 332 PMID: 31291571
Colpaert et al (2005) Nitric oxide relaxes circular smooth muscle of rat distal colon through RhoA/Rho-kinase independent Ca2+ desensitisation. Br J Pharmacol 144 588 PMID: 15655498
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平均评分: 5 (Based on 1 Review.)
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calyculin A for PP1/PP2A (Cal A, 100 nM)