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Forskolin, or coleonol, is a cell-permeable, potent, reversible and rapid activator of adenylyl cyclase, an enzyme that converts ATP to cAMP and pyrophosphate (EC50 = 0.5 μM). In combination with 5 other compounds, forskolin enables chemical reprogramming of mouse embryonic fibroblasts to pluripotent stem cells, without genetic factors: Valproic acid, sodium salt (Cat. No. 2815), RepSox (Cat. No. 3742), Tranylcypromine hydrochloride (Cat. No. 3852), CHIR 99021 (Cat. No. 4423) and 3-Deazaneplanocin A hydrochloride (Cat. No. 4703). In combination with IBMX (Cat. No. 2845), forskolin induces neural differentiation of mesenchymal stem cells by downregulating neuron restrictive silencer factor. In a rat model of Huntington's disease-like neurodegeneration, forskolin also exhibits neuroprotective effects. Hypotensive and vasodilatory agent.
Water-soluble analog, NKH 477 (Cat. No. 1603), and Forskolin synthesized to Ancillary Material Grade also available.
For more information about how Forskolin may be used, see our protocol: Transdifferentiating Fibroblasts into Neurons.
Forskolin is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 410.51. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.25 mM||9.74 mL||48.72 mL||97.44 mL|
|1.25 mM||1.95 mL||9.74 mL||19.49 mL|
|2.5 mM||0.97 mL||4.87 mL||9.74 mL|
|12.5 mM||0.19 mL||0.97 mL||1.95 mL|
References are publications that support the biological activity of the product.
Awad et al (1983) Interactions of forskolin and adenylate cyclase. J.Biol.Chem. 258 2960 PMID: 6681815
Laurenza et al (1989) Forskolin: a specific stimulator of adenylyl cyclase or a diterpene with multiple sites of action? TiPS 10 442 PMID: 2692256
Seamon et al (1983) Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives. J.Med.Chem. 26 436 PMID: 6681845
Kim et al (2005) cAMP induces neuronal differentiation of mesenchymal stem cells via activation of extracellular signal-regulated kinase/MAPK. Neuroreport 16 1357 PMID: 16056139
Hou et al (2013) Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. Science 341 651 PMID: 23868920
Sato et al (2015) SnapShot: Growing Organoids from Stem Cells. Cell 161 1700 PMID: 26091044
Robbins et al (1996) Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J.Med.Chem. 39 2745 PMID: 8709105
If you know of a relevant reference for Forskolin, please let us know.
Keywords: Forskolin, Forskolin supplier, Adenylyl, cyclases, activator, Inositol, cAMP, Signaling, Signalling, adenylate, stem, cells, organoids, coleonol, Cyclase, Enzyme, Substrates, /, Activators, Neural, Stem, Cells, Organoids, 1099, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Forskolin include:
Chan et al (2016) ApoE4 expression accelerates hippocampus-dependent cognitive deficits by enhancing Aβ impairment of Ins signaling in an Alzheimer's disease mouse model. Cell 6 26119 PMID: 27189808
Hook et al (2012) DArgic modulation of ganglion-cell photoreceptors in rat. J Neurosci 35 507 PMID: 22304466
Kaufman et al (2012) Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons. J Neurosci 32 3992 PMID: 22442066
Horváth et al (2012) A new cannabinoid CB2 receptor agonist HU-910 attenuates oxidative stress, inflammation and cell death associated with hepatic ischaemia/reperfusion injury. J Neurosci 165 2462 PMID: 21449982
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
Mo et al (2018) MBD1 Contributes to the Genesis of Acute Pain and Neuropathic Pain by Epigenetic Silencing of Oprm1 and Kcna2 Genes in Primary Sensory Neurons. J Neurosci 38 9883 PMID: 30266739
Noh et al (2018) Specific autophagy and ESCRT components participate in the unconventional secretion of CFTR. Autophagy 14 1761 PMID: 29969945
Gauster et al (2018) Downregulation of p53 drives autophagy during human trophoblast differentiation. Cell Mol Life Sci 75 1839 PMID: 29080089
Avanzato et al (2016) Activation of P2X7 and P2Y11 purinergic receptors inhibits migration and normalizes tumor-derived endothelial cells via cAMP signaling Scientific Reports 6 32602 PMID: 27586846
Cooke et al (2015) Morphine-induced internalization of the L83I mutant of the rat μ-opioid receptor. Cell Death Dis 172 593 PMID: 24697554
Baron et al (2015) The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine. Sci Rep 6 e1629 PMID: 25654762
Ang et al (2015) The short-chain fatty acid receptor GPR43 is transcriptionally regulated by XBP1 in human monocytes. Ann Clin Transl Neurol 5 8134 PMID: 25633224
Walker et al (2015) A second trigeminal CGRP receptor: function and expression of the AMY1 receptor. Nat Commun 2 595 PMID: 26125036
Siuda et al (2015) Optodynamic simulation of β-adrenergic receptor signalling. Eneuro 6 8480 PMID: 26412387
Polito et al (2015) Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3). J Neurosci 2 PMID: 26465004
Zhu et al (2015) Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways. Pharmacol Res Perspect 35 621 PMID: 25589756
Presley et al (2015) Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist. Biochem Pharmacol 3 e00159 PMID: 26196013
Brust et al (2015) New functional activity of aripipr. revealed: Robust antagonism of D2 DA receptor-stimulated Gβγ signaling. Cell Rep 93 85 PMID: 25449598
Ben-Simon et al (2015) A Combined Optogenetic-Knockdown Strategy Reveals a Major Role of Tomosyn in Mossy Fiber Synaptic Plasticity. Pflugers Arch 12 396 PMID: 26166572
Broadbent et al (2015) The cystic fibrosis transmembrane conductance regulator is an extracellular chloride sensor. Sci Rep 467 1783 PMID: 25277268
Muñoz-Llancao et al (2015) Exchange Protein Directly Activated by cAMP (EPAC) Regulates Neuronal Polarization through Rap1B. Biochim Biophys Acta 35 11315 PMID: 26269639
Parnell et al (2015) Phosphorylation of ezrin on Thr567 is required for the synergistic activation of cell spreading by EPAC1 and protein kinase A in HEK293T cells. Mol Metab 1853 1749 PMID: 25913012
Li et al (2015) Increased biogenesis of glucagon-containing secretory granules and glucagon secretion in BIG3-knockout mice. Mol Pharmacol 4 246 PMID: 25737957
Emery et al (2015) Cyclic Adenosine 3',5'-Monophosphate Elevation and Biological Signaling through a Secr. Family Gs-Coupled G Protein-Coupled Receptor Are Restricted to a Single Adenylate Cyclase Isoform. J Cell Mol Med 87 928 PMID: 25769305
Jansen et al (2015) Prostaglandin E2 promotes MYCN non-amplified neuroblastoma cell survival via β-catenin stabilization. Stem Cell Reports 19 210 PMID: 25266063
Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333
Bolognini et al (2012) AM630 behaves as a protean ligand at the human cannabinoid CB2 receptor. Br J Pharmacol 165 2561 PMID: 21615724
Mitra et al (2012) Heterogeneous reallocation of presynaptic efficacy in recurrent excitatory circuits adapting to inactivity. Nat Neurosci 15 250 PMID: 22179109
Korboukh et al (2012) Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice. J Med Chem 55 6467 PMID: 22738238
Tran et al (2012) Dynamic mass redistribution assays decode surface influence on signaling of endogenous purinergic P2Y receptors. Assay Drug Dev Technol 10 37 PMID: 22066912
Buznikov et al (2010) A putative 'pre-nervous' endocannabinoid system in early echinoderm development. Dev Neurosci 32 1 PMID: 19907129
Garavaglia et al (2010) Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates. BMC Neurosci 11 7 PMID: 20085655
Bonetti and Surace (2010) Mouse embryonic retina delivers information controlling cortical neurogenesis. J Mol Cell Cardiol 5 e15211 PMID: 21170332
Post et al (2020) Snake venom gland organoids Cell 180 233 PMID: 31978343
Delpiano et al (2019) Esomeprazole Increases Airway Surface Liquid pH in Primary Cystic Fibrosis Epithelial Cells. Front Pharmacol 9 1462 PMID: 30618754
Sachs et al (2019) Long-term expanding human airway organoids for disease modeling. EMBO J 38 PMID: 30643021
Liu et al (2018) CRISPR-based chromatin remodeling of the endogenous Oct4 or Sox2 locus enables reprogramming to pluripotency. Cell Stem Cell. 22 252 PMID: 29358044
Tozzi et al (2018) DA D2 receptor-mediated neuroprotection in a G2019S Lrrk2 genetic model of Parkinson’s disease. Cell Death Dis 9 204 PMID: 29434188
Li et al (2017) Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression. Theranostics 7 4671 PMID: 29187895
Jewell et al (2019) GPCR signaling inhibits mTORC1 via PKA phosphorylation of Raptor. Elife 8 PMID: 31112131
Saito et al (2019) Establishment of Patient-Derived Organoids and Drug Screening for Biliary Tract Carcinoma. Cell Rep 27 1265 PMID: 31018139
Franchini et al (2019) Linking NMDA Receptor Synaptic Retention to Synaptic Plasticity and Cognition. iScience 19 927 PMID: 31518901
French et al (2019) Dual-Mode FRET and BRET Sensors for Detecting cAMP Dynamics. ACS Omega 4 15504 PMID: 31572851
Schnúr et al (2019) Phosphorylation-dependent modulation of CFTR macromolecular signalling complex activity by cigarette smoke condensate in airway epithelia. Sci Rep 9 12706 PMID: 31481727
Pattabiraman et al (2016) Activation of PKA leads to mesenchymal-to-epithelial transition and loss of tumor-initiating ability. Science 351 aad3680 PMID: 26941323
Havekes et al (2016) Compartmentalized PDE4A5 Signaling Impairs Hippocampal Synaptic Plasticity and Long-Term Memory. J Neurosci 36 8936 PMID: 27559174
Moon et al (2015) Compartmentalized accumulation of cAMP near complexes of multidrug resistance protein 4 (MRP4) and cystic fibrosis transmembrane conductance regulator (CFTR) contributes to drug-induced diarrhea. J Biol Chem 290 11246 PMID: 25762723
Chen et al (2011) Dual Phosphorylation of suppressor of fused (Sufu) by PKA and GSK3beta regulates its stability and localization in the primary cilium. J Biol Chem 286 13502 PMID: 21317289
Benito et al (2011) cAMP response element-binding protein is a primary hub of activity-driven neuronal gene expression. J Neurosci 31 18237 PMID: 22171029
Althaus et al (2011) Nitric oxide inhibits highly selective sodium channels and the Na+/K+-ATPase in H441 cells. Am J Respir Cell Mol Biol 44 53 PMID: 20139350
Hosoi et al (2002) Identification of a novel human eicosanoid receptor coupled to G(i/o). J Biol Chem 277 31459 PMID: 12065583
Segal et al (2019) Single cell analysis of human foetal liver captures the transcriptional profile of hepatobiliary hybrid progenitors. Nat Commun 10 3350 PMID: 31350390
Garcia et al (2019) Huntington's Disease Patient-Derived Astrocytes Display Electrophysiological Impairments and Reduced Neuronal Support. Front Neurosci 13 669 PMID: 31316341
Chiu et al (2019) NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content. Cell Rep 28 332 PMID: 31291571
Cordonier et al (2019) Luciferase Reporter Mice for In Vivo Monitoring and Ex Vivo Assessment of Hypothalamic Signaling of Socs3 Expression. J Endocr Soc 3 1246 PMID: 31214662
Luo (2017) β2-adrenoreceptor Inverse Agonist Down-regulates Muscarine Cholinergic Subtype-3 Receptor and Its Downstream Signal Pathways in Airway Smooth Muscle Cells in vitro. Scientific Reports 7 39905 PMID: 28051147
Belgacem and Borodinsky (2015) Inversion of Sonic hedgehog action on its canonical pathway by electrical activity. Eur J Neurosci 112 4140 PMID: 25829542
Shelton et al (2014) Derivation and expansion of PAX7-positive muscle progenitors from human and mouse embryonic stem cells. Br J Pharmacol 3 516 PMID: 25241748
Felizola et al (2014) PCP4: a regulator of aldosterone synthesis in human adrenocortical tissues. Glia 52 159 PMID: 24403568
Yang et al (2014) PKA catalytic subunit compartmentation regulates contractile and hypertrophic responses to β-adrenergic signaling. J Biol Chem 66 83 PMID: 24225179
Jia et al (2013) Age-dependent regulation of synaptic connections by DA D2 receptors. Nat Neurosci 16 1627 PMID: 24121738
Ehrlich et al (2013) Prostaglandin E receptor EP1 forms a complex with DA D1 receptor and directs D1-induced cAMP production to adenylyl cyclase 7 through mobilizing G(βγ) subunits in human embryonic kidney 293T cells. Mol Pharmacol 84 476 PMID: 23842570
Pale et al (2013) Cyclic AMP stimulates neurite outgrowth of lamprey reticulospinal neurons without substantially altering their biophysical properties. Neuroscience 245 74 PMID: 23603516
Wiseman et al (2013) Proteasomal degradation of eukaryotic elongation factor-2 kinase (EF2K) is regulated by cAMP-PKA signaling and the SCFβTRCP ubiquitin E3 ligase. J Biol Chem 288 17803 PMID: 23640883
Roscioni et al (2009) PKA and Epac cooperate to augment bradykinin-induced interleukin-8 release from human airway smooth muscle cells. Respir Res 10 88 PMID: 19788733
Byrnes et al (2009) Metabotropic glutamate receptor 5 activation inhibits microglial associated inflammation and neurotoxicity. J Clin Invest 57 550 PMID: 18816644
Al-Taei et al (2017) Prostaglandin E2-mediated adenosinergic effects on CD14+ cells: Self-amplifying immunosuppression in cancer. Oncoimmunology 6 e1268308 PMID: 28344879
Burgueño et al (2017) A Complementary Scale of Biased Agonism for Agonists with Differing Maximal Responses. Sci Rep 7 15389 PMID: 29133887
Yang et al (2017) Derivation of Pluripotent Stem Cells with In Vivo Embryonic and Extraembryonic Potency. Cell 169 243 PMID: 28388409
Demeautis et al (2017) Multiplexing PKA and ERK12 kinases FRET biosensors in living cells using single excitation wavelength dual colour FLIM. Sci Rep 7 41026 PMID: 28106114
Brzosko et al (2015) Retroactive modulation of spike timing-dependent plasticity by DA. Elife 4 PMID: 26516682
Elliott et al (2015) Somatostatin and Ins mediate glucose-inhibited glucagon secretion in the pancreatic α-cell by lowering cAMP. Am J Physiol Endocrinol Metab 308 E130 PMID: 25406263
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Chou et al (2014) Prostaglandin E2 promotes features of replicative senescence in chronically activated human CD8+ T cells. PLoS One 9 e99432 PMID: 24918932
Vandame et al (2014) The spatio-temporal dynamics of PKA activity profile during mitosis and its correlation to chromosome segregation. Cell Cycle 13 3232 PMID: 25485503
Muthusamy et al (2014) A method to identify and isolate pluripotent human stem cells and mouse epiblast stem cells using lipid body-associated retinyl ester fluorescence. Stem Cell Reports 3 169 PMID: 25068130
Adelfinger et al (2014) GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization. Biochem Pharmacol 91 369 PMID: 25065880
Tao et al (2013) cAMP level modulates scleral collagen remodeling, a critical step in the development of myopia. Br J Pharmacol 8 e71441 PMID: 23951163
Sohn et al (2013) Melanocortin 4 receptors reciprocally regulate sympathetic and parasympathetic preganglionic neurons. J Mol Endocrinol 152 612 PMID: 23374353
Patra et al (2018) Mutant GNAS drives pancreatic tumourigenesis by inducing PKA-mediated SIK suppression and reprogramming lipid metabolism. Nat Cell Biol 20 811 PMID: 29941929
Costa et al (2018) Activation of Serotonin 5-HT7 Receptors Modulates Hippocampal Synaptic Plasticity by Stimulation of Adenylate Cyclases and Rescues Learning and Behavior in a Mouse Model of Fragile X Syndrome. Front Mol Neurosci 11 353 PMID: 30333723
Ford et al (2018) A Cell/Cilia Cycle Biosensor for Single-Cell Kinetics Reveals Persistence of Cilia after G1/S Transition Is a General Property in Cells and Mice. Dev Cell 47 509 PMID: 30458140
Aguileta et al (2016) A siRNA screen reveals the prosurvival effect of protein kinase A activation in conditions of unresolved endoplasmic reticulum stress. Cell Death Differ 23 1670 PMID: 27341185
Schapitz et al (2010) Neuroligin 1 is dynamically exchanged at postsynaptic sites. J Neurosci 30 12733 PMID: 20861378
Goffin et al (2010) DA-dependent tuning of striatal inhibitory synaptogenesis. PLoS One 30 2935 PMID: 20181591
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Culturing liver organoids - used to swell the organoids
Jurkat cells were treated with different concentration of Forskolin for 15 minutes and the cAMP was measured (the cAMP levels are reversely correlated with Luminescent values.)
10 μM for 30min
To start reprogramming, cultures were switched to reprogramming medium (ES medium supplemented with 10 mM Parnate, 3 mM Chir99021, 1 mM A83-01, and 10 mM Forskolin)
HEK293 cells transfected with cAMP FRET sensor, Epac-S(H187) were perfused in normal tyrode solution and excited alternately at 430 nm and fluorescence was captured at 470 and 535 nm. Forskolin (10 µM) was added at 1 min to activate adenylyl cyclase and increase intracellular cAMP, which is detected as an increase in 470/535 fluorescence ratio.
Forskolin activates adenylyl cyclase and increases intracellular cAMP. We used at 10 microM in cultured astrocytes to increase intracellular cAMP level.
The following protocols feature additional information for the use of Forskolin (Cat. No. 1099).
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.