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Forskolin

Catalog No. T2939 CAS 66575-29-9

Synonyms: 毛喉素, Coleonol, Colforsin

Forskolin, a potent activator of the adenylate cyclase (EC50: 0.5 μM), can increase the cAMP level. It is extracted from the plant Coleus forskohlii.

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Forskolin, CAS 66575-29-9

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Purity: 98%

Biological Description

Chemical Properties

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Description	Forskolin, a potent activator of the adenylate cyclase (EC50: 0.5 μM), can increase the cAMP level. It is extracted from the plant Coleus forskohlii.
Targets&IC50	Adenylyl cyclase:0.5 μM (cell free)
In vitro	Forskolin (Fsk) treatment inhibited the proliferation of both Kit 225 and MT-2 cells in a dose-dependent manner with an IC50 equal to ～5 μM Forskolin. Fsk treatment (10–100 μM) increased cAMPi levels ～5- to 20-fold above basal levels, which reached maximum levels between 50–100 μM Fsk [2]. Forskolin binds to adenylyl cyclase in membranes from stably transfected Sf9 cells expressing type 1 adenylyl cyclase with an IC50 value of 41 nM and demonstrates an EC50 value of 0.5 μM in an activation assay assessing formation of cAMP from ATP [1]. "VC6T" [VPA, CHIR99021 (CHIR), 616452, Tranylcypromine] plus Forskolin (VC6TF) induced some GFP-positive clusters expressing E-cadherin [3].
In vivo	The Mrp4(-/-) mice exhibited no overt abnormalities in the development of the retinal vasculature, but retinal vascular development in the Mrp4(-/-) mice was suppressed in response to forskolin administration. The forskolin-treated Mrp4(-/-) mice showed an increased number of Ki67-positive and cleaved caspase 3-positive ECs, a significant decrease in the amount of pericyte coverage, and a reduced number of empty sleeves. In pups exposed to hyperoxia (75% oxygen) from P7 to P12, the Mrp4(-/-) mice showed a significant increase in the unvascularized retinal area [4]. Hepatic fibrosis induced by CCl4 was significantly reduced by forskolin, as indicated by decreased α-SMA expression and collagen deposition. Forskolin co-treatment significantly attenuated oxidative stress and inflammation, reduced TGF-β1 levels and down-regulated mRNA expression of Ptch-1, Smo and Gli-2 through cAMP-dependent PKA activation [5].
Kinase Assay	For Jak3 kinase assays, Fsk-treated MT-2 cells were lysed, clarified, and immunoprecipitated using Jak3 antibody as described above. Kinase reactions were carried out as described previously at 30 °C for 20 min. For PKA kinase assays, untreated MT-2 cells were lysed, and Jak3 was immunoprecipitated and bound to PAS beads as described previously. Immunoprecipitated Jak3 was washed with kinase buffer (50 mM Hepes-NaOH (pH 7.4), 10 mM MgCl2, 0.5 mM EGTA, 0.5 mM DTT, 20 μg/ml aprotinin, 10 μg/ml leupeptin, 1 μg/ml pepstatin A) and incubated with 200 μM ATP and purified protein kinase A catalytic subunit (PKAc) as indicated in the figure legends. Kinase reactions were carried out at 32 °C for 30 min followed by vigorous washing of the beads with cold kinase wash buffer as described previously. For [γ-32P]ATP radiolabeled kinase assays using recombinant Jak3, Hek293 cells were transfected with wild type (WT) Jak3 or kinase-dead Jak3 K855A using Lipofectamine 2000 according to the manufacturer's instructions. Cells were lysed and immunoprecipitated with Jak3 antibody. Jak3-bound PAS beads were washed three times in cold lysis buffer followed by kinase buffer. Kinase reactions were initiated by adding 10 μCi [γ-32P]ATP, 10 μm unlabeled ATP, and 1 μg of purified PKAc to Jak3-bound PAS bead reaction mixtures. Kinase reactions were performed at 32 °C for 30 min. Jak3-bound PAS beads were washed three times in radioimmunoassay buffer (10 mM Tris-HCl, pH 7.4, 75 mM NaCl, 20 mM EDTA, 10 mM EGTA, 20 mM Na4P2O7, 50 mM NaF, 20 mM 2-glycerolphosphate, 1 mM p-nitrophenyl phosphate, 0.1% Triton X-100) and one time in kinase wash buffer. The reactions were stopped by adding 2× SDS-PAGE sample buffer followed by SDS-PAGE. Coomassie stainable Jak3 bands were excised from the PVDF membrane and subjected to phosphoamino acid analysis [2].
Cell Research	Kit 225 or MT-2 cells were treated with 1, 5, 10, 20, 50, or 100 μM Forskolin for 20 min at 37 °C. Cells were lysed and clarified by centrifugation, and the concentration of cAMP was detected by direct cAMP ELISA. Optical density was measured at 405 nm, and the concentration of intracellular cAMP was calculated using a weighted four parameter logistic curve according to the manufactures instructions [2].
Animal Research	Forskolin was dissolved in dimethyl sulfoxide (DMSO) and injected intraperitoneally into neonatal mice at postnatal days 4 (P4) and 5 (P5). Mice injected with DMSO served as the controls. The treated mice were euthanized at P6, and their retinas were isolated for whole-mount immunohistochemistry (IHC). We first tested the effect of different concentrations of forskolin on the survival rate and retinal vasculature and determined the optimal concentration, 1.0 μg/50 μL (0.3 mg/kg) at P4 and 1.5 μg/50 μL (0.5 mg/kg) at P5, used to compare the retinal vascular phenotypes between WT mice and Mrp4-deficient mice [4]. . After acclimatization for 2 weeks, animals were randomly divided into four groups of eight rats each and treated for six consecutive weeks as follows: The first group was treated with CCl4 (50% CCl4/corn oil; 0.5 mL·kg?1, i.p.) twice a week to induce liver fibrosis. The second group was given forskolin only at a dose of 10 mg·kg?1, i.p., dissolved in a DMSO/saline solution (1:49) five times a week. The third group was given both CCl4 and forskolin. The dose of forskolin used here was based on the results of our preliminary study. The fourth group served as the normal control, receiving vehicles only. At 24 h after the last injection, blood samples were collected from the retro‐orbital plexus after light anesthesia with sodium pentobarbital (50 mg·kg?1, i.p.). Serum was separated by centrifugation at 3000× g for 10 min and was used for the assessment of liver functions. Rats were killed by cervical dislocation, and livers were removed and weighed. A portion of liver tissue was washed and homogenized to obtain a 20% (w·v?1) homogenate, which was used for assessment of oxidative stress, inflammatory and fibrogenic markers. Another portion was placed in formalin for immunohistochemical and histopathological analyses. The remainder was stored at ?80°C, together with the 20% homogenate, until needed [5].

Synonyms	毛喉素, Coleonol, Colforsin
Molecular Weight	410.507
Formula	C22H34O7
CAS No.	66575-29-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: Insoluble

DMSO: 30 mg/mL (73 mM)

Ethanol: 15 mg/mL (36.5 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Robbins JD, et al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem. 1996 Jul 5;39(14):2745-52. 2. Rodriguez G, et al. Forskolin-inducible cAMP pathway negatively regulates T-cell proliferation by uncoupling the interleukin-2 receptor complex. J Biol Chem. 2013 Mar 8;288(10):7137-46. 3. Hou P, et al. Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. Science. 2013 Aug 9;341(6146):651-4. 4. Matsumiya W, et al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53(13):8029-35. 5. El-Agroudy NN, et al. Forskolin, a hedgehog signalling inhibitor, attenuates carbon tetrachloride-induced liver fibrosis in rats. Br J Pharmacol. 2016 Nov;173(22):3248-3260. 6. Lu J, Dou F, Yu Z. The potassium channel KCa3. 1 represents a valid pharmacological target for microgliosis-induced neuronal impairment in a mouse model of Parkinson’s disease[J]. Journal of Neuroinflammation. 2019, 16(1): 1-14. 7. Lin J Y, Cheng J, Du Y Q, et al. In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals[J]. Cell Discovery. 2020, 6(1): 1-12. 8. Lin J Y, Cheng J, Du Y Q, et al. In vitro pancreatic islet cluster expansion facilitated by hormones and chemicals[J]. Cell Discovery. 2020, 6(1): 1-12. 9. Wu L, Dong A, Dong L, et al. PARIS, an optogenetic method for functionally mapping gap junctions[J]. eLife. 2019 Jan 14;8. pii: e43366. 10. Xiaoli F, Yaqing Z, Ruhui L, et al. Graphene oxide disrupted mitochondrial homeostasis through inducing intracellular redox deviation and autophagy-lysosomal network dysfunction in SH-SY5Y cells[J]. Journal of Hazardous Materials. 2021: 126158.

Citations

1. Ma X, Lu Y, Zhou Z, Human expandable pancreatic progenitor–derived β cells ameliorate diabetes. Science Advances. 2022, 8(8): eabk1826. 2. Xiaoli F, Yaqing Z, Ruhui L, et al. Graphene oxide disrupted mitochondrial homeostasis through inducing intracellular redox deviation and autophagy-lysosomal network dysfunction in SH-SY5Y cells. Journal of Hazardous Materials. 2021: 126158. 3. Wang W, Ren S, Lu Y, et al. Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production. The EMBO Journal. 2021 Jun 1;40(11):e106771. doi: 10.15252/embj.2020106771. Epub 2021 Apr 28. 4. Wu L, Dong A, Dong L, et al. PARIS, an optogenetic method for functionally mapping gap junctions. ELife. 2019 Jan 14;8. pii: e43366 5. Lin J Y, Cheng J, Du Y Q, et al. In vitro pancreatic islet cluster expansion facilitated by hormones and chemicals. Cell Discovery. 2020, 6(1): 1-12 6. Zhao C, Sun C, Yuan J, et al. Hericium caput-medusae (Bull.: Fr.) Pers. fermentation concentrate polysaccharides improves intestinal bacteria by activating chloride channels and mucus secretion. Journal of Ethnopharmacology. 2022: 115721. 7. Miao Y, Zhang Y, Qiao S, et al. Oral administration of curcumin ameliorates pulmonary fibrosis in mice through 15d-PGJ2-mediated induction of hepatocyte growth factor in the colon. Acta Pharmacologica Sinica. 2020: 1-14 8. Lin J Y, Cheng J, Du Y Q, et al. In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals. Cell Discovery. 2020, 6(1): 1-12 9. Jin C, Zhao S, Xie H. Forskolin enhanced the osteogenic differentiation of human dental pulp stem cells in vitro and in vivo. Journal of Dental Sciences. 2022 10. Wang H, Liang N, Huang D, et al. The effects of high-density lipoprotein and oxidized high-density lipoprotein on forskolin-induced syncytialization of BeWo cells. Placenta. 2021, 103: 199-205

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Keywords

Forskolin 66575-29-9 代谢神经科学自噬 AChR Adenylyl cyclase Autophagy FXR notropic pregnane Inhibitor exosome cancer antihypertensive antiaggregatory X receptor prostate NR1H4 Adenylate Cyclase PXR cAMP inhibit Colforsin Coleonol inhibitor

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