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Submit ReviewChelerythrine chloride is a cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP. Has a wide range of biological activities, including antiplatelet, anti-inflammatory, antibacterial and antitumor effects. Activates MAPK pathways, independent of PKC inhibition. Inhibits binding of BclXL to Bak (IC50 = 1.5 μM) or Bad proteins and stimulates apoptosis.
分子量 | 383.83 |
公式 | C21H18ClNO4 |
储存 | Desiccate at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 3895-92-9 |
PubChem ID | 72311 |
InChI Key | WEEFNMFMNMASJY-UHFFFAOYSA-M |
Smiles | C[N+](C3=C2C=CC4=C3C=C(OCO5)C5=C4)=CC1=C2C=CC(OC)=C1OC.[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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 3.84 | 10 | |
DMSO | 3.84 | 10 |
以下数据基于产品分子量 383.83。 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 |
---|---|---|---|
0.1 mM | 26.05 mL | 130.27 mL | 260.53 mL |
0.5 mM | 5.21 mL | 26.05 mL | 52.11 mL |
1 mM | 2.61 mL | 13.03 mL | 26.05 mL |
5 mM | 0.52 mL | 2.61 mL | 5.21 mL |
参考文献是支持产品生物活性的出版物。
Chan et al (2003) Identification of chelerythrine as an inhibitor of BclXL function. J.Biol.Chem. 278 20453 PMID: 12702731
Herbert et al (1990) Chelerythrine is a potent and specfic inhibitor of protein kinase C. Biochem.Biophys.Res.Commun. 172 993 PMID: 2244923
Lee et al (1998) Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C. J.Biol.Chem. 273 19829 PMID: 9677417
Yu et al (2000) Activation of p38 and c-Jun N-terminal kinase pathways and induction of apoptosis by chelerythrine do not require inhibition of protein kinase C. J.Biol.Chem. 275 9612 PMID: 10734112
If you know of a relevant reference for Chelerythrine chloride, please let us know.
关键词: Chelerythrine chloride, Chelerythrine chloride supplier, Potent, protein, kinase, C, inhibitors, inhibits, PKC, Kinases, Protein, Kinase, 1330, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Chelerythrine chloride 的部分引用包括:
Cho et al (2012) Pituitary adenylate cyclase-activating polypeptide induces postsynaptically expressed potentiation in the intra-amygdala circuit. J Neurosci 32 14165 PMID: 23055486
Fuortes et al (2010) Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation. Epilepsia 51 1633 PMID: 20659148
Jin and Yu (2010) Involvement of protein kinase C in mor. tolerance at spinal levels of rats. Autophagy 1 122 PMID: 22778820
Livingstone et al (2019) Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons. Front Mol Neurosci 12 198 PMID: 31474829
Martín-Segura et al (2019) Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism. Front Neurol 10 675 PMID: 31293510
Liu and Zhuo (2014) Loss of long-term depression in the insular cortex after tail amputation in adult mice. Mol Pain 10 1 PMID: 24398034
Song et al (2010) Involvement of protein kinase C-CPI-17 in androgen modulation of angiotensin II-renal vasoconstriction. ACS Chem Neurosci 85 614 PMID: 19797427
Morelli et al (2014) Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation. BMC Cancer 14 921 PMID: 25481381
Mockett et al (2011) Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus. J Neurosci 31 7380 PMID: 21593322
Xu et al (2009) Increases in transient receptor potential vanilloid-1 mRNA and protein in primary afferent neurons stimulated by protein kinase C and their possible role in neurogenic inflammation. Cardiovasc Res 87 482 PMID: 18752301
Ortinski et al (2015) Cocaine-seeking is associated with PKC-dependent reduction of excitatory signaling in accumbens shell D2 DA receptor-expressing neurons. Neuropharmacology 92 80 PMID: 25596492
Most et al (2013) S100A1 deficiency impairs postischemic angiogenesis via compromised proangiogenic endothelial cell function and nitric oxide synthase regulation. Circ Res 112 66 PMID: 23048072
Gosselin et al (2013) Extracellular microvesicles from astrocytes contain functional glutamate transporters: regulation by protein kinase C and cell activation. Front Cell Neurosci 7 251 PMID: 24368897
Chen et al (2011) mGluR5 positive modulators both potentiate activation and restore inhibition in NMDA receptors by PKC dependent pathway. J Biomed Sci 18 19 PMID: 21342491
Xie and Wang (2009) Ablation of transient receptor potential vanilloid 1 abolishes endothelin-induced increases in afferent renal nerve activity: mechanisms and functional significance. Hypertension 54 1298 PMID: 19858408
Xu et al (2010) The effects of sympathetic outflow on upregulation of vanilloid receptors TRPV(1) in primary afferent neurons evoked by intradermal capsaicin. Exp Neurol 222 93 PMID: 20036240
Li (2017) Involvement of galanin and galanin receptor 1 in nociceptive modulation in the central nucleus of amygdala in normal and neuropathic rats. Sci Rep 7 15317 PMID: 29127424
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