K252a | Alomone Labs K-150 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

K252a

catalog :

K-150

more info or order :

Alomone Labs product webpage

citations: 34

Reference
Garad M, Edelmann E, Leßmann V. Long-term depression at hippocampal mossy fiber-CA3 synapses involves BDNF but is not mediated by p75NTR signaling. Sci Rep. 2021;11:8535 pubmed publisher
Yi L, Zhu J, Dong S, Li C, Zhang Q, Cheng J, et al. miR-34a induces spine damages via inhibiting synaptotagmin-1 in depression. Neurobiol Stress. 2020;13:100243 pubmed publisher
Guerenne Del Ben T, Couderc V, Duponchel L, Sol V, Leproux P, Petit J. Multiplex coherent anti-Stokes Raman scattering microspectroscopy detection of lipid droplets in cancer cells expressing TrkB. Sci Rep. 2020;10:16749 pubmed publisher
Jiang Y, Fu P, Liu Y, Wang C, Zhao P, Chu X, et al. Near-infrared light-triggered NO release for spinal cord injury repair. Sci Adv. 2020;6: pubmed publisher
Ding B, Dobner P, Mullikin Kilpatrick D, Wang W, Zhu H, Chow C, et al. BDNF Activates an NFI-Dependent Neurodevelopmental Timing Program By Sequestering NFATc4. Mol Biol Cell. 2018;: pubmed publisher
Abbaci A, Talbot H, Saada S, Gachard N, Abraham J, Jaccard A, et al. Neurotensin receptor type 2 protects B-cell chronic lymphocytic leukemia cells from apoptosis. Oncogene. 2017;: pubmed publisher
Mazouffre C, Geyl S, Perraud A, Blondy S, Jauberteau M, Mathonnet M, et al. Dual inhibition of BDNF/TrkB and autophagy: a promising therapeutic approach for colorectal cancer. J Cell Mol Med. 2017;21:2610-2622 pubmed publisher
Kawamoto M, Onishi H, Ozono K, Yamasaki A, Imaizumi A, Kamakura S, et al. Tropomyosin-related kinase B mediated signaling contributes to the induction of malignant phenotype of gallbladder cancer. Oncotarget. 2017;8:36211-36224 pubmed publisher
Trubiani O, Guarnieri S, Diomede F, Mariggio M, Merciaro I, Morabito C, et al. Nuclear translocation of PKC? isoenzyme is involved in neurogenic commitment of human neural crest-derived periodontal ligament stem cells. Cell Signal. 2016;28:1631-41 pubmed publisher
Mu R, Fang X, Wang S, Li C, Chen S, Chen X, et al. Antidepressant-like effects of standardized gypenosides: involvement of brain-derived neurotrophic factor signaling in hippocampus. Psychopharmacology (Berl). 2016;233:3211-21 pubmed publisher
Jiang B, Song L, Wang C, Zhang W, Huang C, Tong L. Antidepressant-Like Effects of GM1 Ganglioside Involving the BDNF Signaling Cascade in Mice. Int J Neuropsychopharmacol. 2016;19: pubmed publisher
Dubanet L, Bentayeb H, Petit B, Olivrie A, Saada S, de la Cruz Morcillo M, et al. Anti-apoptotic role and clinical relevance of neurotrophins in diffuse large B-cell lymphomas. Br J Cancer. 2015;113:934-44 pubmed publisher
Igelhorst B, Niederkinkhaus V, Karus C, Lange M, Dietzel I. Regulation of neuronal excitability by release of proteins from glial cells. Philos Trans R Soc Lond B Biol Sci. 2015;370: pubmed publisher
Jiang B, Huang C, Chen X, Tong L, Zhang W. Tetramethylpyrazine Produces Antidepressant-Like Effects in Mice Through Promotion of BDNF Signaling Pathway. Int J Neuropsychopharmacol. 2015;18: pubmed publisher
Jiang B, Wang F, Yang S, Fang P, Deng Z, Xiao J, et al. SKF83959 produces antidepressant effects in a chronic social defeat stress model of depression through BDNF-TrkB pathway. Int J Neuropsychopharmacol. 2014;18: pubmed publisher
Kolarow R, Kuhlmann C, Munsch T, Zehendner C, Brigadski T, Luhmann H, et al. BDNF-induced nitric oxide signals in cultured rat hippocampal neurons: time course, mechanism of generation, and effect on neurotrophin secretion. Front Cell Neurosci. 2014;8:323 pubmed publisher
Ly K, Régent A, Molina E, Saada S, Sindou P, Le Jeunne C, et al. Neurotrophins are expressed in giant cell arteritis lesions and may contribute to vascular remodeling. Arthritis Res Ther. 2014;16:487 pubmed publisher
Larios J, Jausoro I, Benítez M, Bronfman F, Marzolo M. Neurotrophins regulate ApoER2 proteolysis through activation of the Trk signaling pathway. BMC Neurosci. 2014;15:108 pubmed publisher
Schulz Klaus B, Lessmann V, Endres T. BDNF-dependent consolidation of fear memories in the perirhinal cortex. Front Behav Neurosci. 2013;7:205 pubmed publisher
Kimura Y, Fujita Y, Shibata K, Mori M, Yamashita T. Sigma-1 receptor enhances neurite elongation of cerebellar granule neurons via TrkB signaling. PLoS ONE. 2013;8:e75760 pubmed publisher
Fujita Y, Sato A, Yamashita T. Brimonidine promotes axon growth after optic nerve injury through Erk phosphorylation. Cell Death Dis. 2013;4:e763 pubmed publisher
Ovejero Benito M, Frade J. Brain-derived neurotrophic factor-dependent cdk1 inhibition prevents G2/M progression in differentiating tetraploid neurons. PLoS ONE. 2013;8:e64890 pubmed publisher
Odate S, Nakamura K, Onishi H, Kojima M, Uchiyama A, Nakano K, et al. TrkB/BDNF signaling pathway is a potential therapeutic target for pulmonary large cell neuroendocrine carcinoma. Lung Cancer. 2013;79:205-14 pubmed publisher
Chapleau C, Pozzo Miller L. Divergent roles of p75NTR and Trk receptors in BDNF's effects on dendritic spine density and morphology. Neural Plast. 2012;2012:578057 pubmed publisher
Jiang B, Xiong Z, Yang J, Wang W, Wang Y, Hu Z, et al. Antidepressant-like effects of ginsenoside Rg1 are due to activation of the BDNF signalling pathway and neurogenesis in the hippocampus. Br J Pharmacol. 2012;166:1872-87 pubmed publisher
Meis S, Endres T, Lessmann V. Postsynaptic BDNF signalling regulates long-term potentiation at thalamo-amygdala afferents. J Physiol. 2012;590:193-208 pubmed publisher
Akil H, Perraud A, Mélin C, Jauberteau M, Mathonnet M. Fine-tuning roles of endogenous brain-derived neurotrophic factor, TrkB and sortilin in colorectal cancer cell survival. PLoS ONE. 2011;6:e25097 pubmed publisher
Tomokiyo A, Maeda H, Fujii S, Monnouchi S, Wada N, Kono K, et al. A multipotent clonal human periodontal ligament cell line with neural crest cell phenotypes promotes neurocytic differentiation, migration, and survival. J Cell Physiol. 2012;227:2040-50 pubmed publisher
Fujita Y, Endo S, Takai T, Yamashita T. Myelin suppresses axon regeneration by PIR-B/SHP-mediated inhibition of Trk activity. EMBO J. 2011;30:1389-401 pubmed publisher
Harada C, Guo X, Namekata K, Kimura A, Nakamura K, Tanaka K, et al. Glia- and neuron-specific functions of TrkB signalling during retinal degeneration and regeneration. Nat Commun. 2011;2:189 pubmed publisher
Kondo Y, Saruta J, To M, Shiiki N, Sato C, Tsukinoki K. Expression and Role of the BDNF Receptor-TrkB in Rat Adrenal Gland under Acute Immobilization Stress. Acta Histochem Cytochem. 2010;43:139-47 pubmed publisher
Tey H, Yosipovitch G. Targeted treatment of pruritus: a look into the future. Br J Dermatol. 2011;165:5-17 pubmed publisher
Butowt R, von Bartheld C. Fates of neurotrophins after retrograde axonal transport: phosphorylation of p75NTR is a sorting signal for delayed degradation. J Neurosci. 2009;29:10715-29 pubmed publisher
Tsunoda S, Okumura T, Ito T, Mori Y, Soma T, Watanabe G, et al. Significance of nerve growth factor overexpression and its autocrine loop in oesophageal squamous cell carcinoma. Br J Cancer. 2006;95:322-30 pubmed

image

image 1 :

Alomne Labs K252a inhibits MARCKS phosphorylation via PKC in C6 glioma cells. - Cells were grown to 70% confluence and then serum starved for 18 h. The cells were preincubated for 30 min with different concentrations ofK252a(#K-150) and stimulated with 2 MPMA(#P-800) for 30 min. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho (ser)-MARCKS (myristoylated alanin-rich protein kinase C substrate).

image 2 :

Alomone Labs K252a inhibits NGF-mediated survival of serum-deprived PC12 cells. - Dose-response curve ofK252a(#K-150) inhibition of the 100 ng/mlNative mouse NGF 2.5S protein ( 95%)(#N-100) mediated survival of serum-deprived PC12 cells. IC50was determined at 23.7 nM.

product information

CAT :

K-150

SKU :

K-150_0.1 mg

Product Name :

K252a

Group Type :

Non Antibodies

Product Type :

S. Molecules

Storage After Reconstitution :

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Shipping and storage :

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

Product Page - Scientific background :

K252a is an alkaloid isolated from Nocardiopisis sp. soil fungi. This ATP analogue is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50= 1.8 and 1.7 nM respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nM).1-8It is reported to promote myogenic differentiation in C2 mouse myoblasts5 and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity.9 Paradoxically K252a exerts neurotrophic effects on primary sensory neurons, neuroblastoma cells, PC12 cells, and central neurons.10,11

Supplier :

Alomone Labs

Target :

Protein kinases

Long Description :

K252a (#K-150) is a highly pure, natural, and biologically active compound.

Short Description :

A Potent Inhibitor of Protein Kinase A, Protein Kinase C, and Protein Kinase G

MW :

467.5

Synonyms :

SF 2370

Source :

Natural

Molecular formula :

C27H21N3O5.

Effective Concentration :

10-200 nM.

Activity :

K252a inhibits a variety of kinases including PKC (IC50 = 25 nM), PKA (IC50 = 18 nM) and PKG (IC50 = 20 nM)1. It also inhibits CaMK (IC50 = 1.8 nM) and MLCK (IC50 = 17 nM). K252a has also been shown to inhibit NGF mediated proliferation through the Trk receptor family2.

Reconstitution and Solubility :

DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Solubility :

DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions :

Up to one week at 4°C or three months at -20°C.Protect from light.

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Applications key :

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Purity :

>98%

CAS No :

97161-97-2

Form :

Lyophilized Powder

Comment :

Contact Alomone Labs for technical support and product customization

UNSPSC :

41116134

Bioassay Tested :

Yes

Chemical Name :

9,12-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9alpha,10beta,12alpha)-.

more info or order :

Alomone Labs product webpage