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Forskolin

Catalog No. T2939   CAS 66575-29-9
Synonyms: Coleonol, Colforsin

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Forskolin Chemical Structure
Forskolin, CAS 66575-29-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 36.00
10 mg In stock $ 51.00
25 mg In stock $ 79.00
50 mg In stock $ 97.00
100 mg In stock $ 147.00
200 mg In stock $ 192.00
500 mg In stock $ 323.00
1 mL * 10 mM (in DMSO) In stock $ 51.00
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Purity: 99.86%
Purity: 99.72%
Purity: 99.57%
Purity: 99.57%
Purity: 99.57%
Purity: 99.57%
Purity: 98.83%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.
Targets&IC50 Adenylyl cyclase:0.5 μM (cell free)
In vitro METHODS: Rat adrenal medullary chromosomal tumor cells PC12 were treated with Forskolin (0.01-10 µM) for 3-48 h. The growth inhibition of the cells was detected by MTT.
RESULTS: The cell viability decreased rapidly after treatment with 10 µM Forskolin (88.4% after 6 h and 60.5% after 48 h). [1]
METHODS: Human myeloma cells U266, H929, INA-6, RPMI 8226 and OPM-2 were treated with Forskolin (1-100 µM) for 72 h. Cell death was detected by Flow Cytometry.
RESULTS: Forskolin dose-dependently induced cell death in human myeloma cells, with U266, OPM-2 and INA-6 being more sensitive than H929 and RPMI 8226 cells. [2]
METHODS: Human IL-2-dependent leukemia cells Kit 225 and human leukemia cells MT-2 were treated with Forskolin (1-100 μM) for 20 min, and cAMP concentration was measured by ELISA.
RESULTS: Forskolin induced an up-regulation of cAMP levels, which reached a maximum level between 50-100 μm. [3]
In vivo METHODS: To assay anti-tumor activity in vivo, Forskolin (4-5 mg/kg in PBS/DMSO solution (15:1)) was injected intraperitoneally into BALB/c nude mice bearing murine multiple myeloma tumor MOPC315, and was administered on the 2nd/4th/6th day after tumor cell injection.
RESULTS: All mice eventually developed tumors, but Forskolin significantly delayed tumor growth in vivo. Compounds that increase cAMP may have therapeutic potential in the treatment of multiple myeloma. [4]
METHODS: To investigate the effect of Forskolin on retinal inflammation under diabetic conditions, Forskolin (50 mg/kg) was administered by gavage once weekly for twelve weeks to C57BL/6 mice in the STZ-induced diabetes model.
RESULTS: Retinal glucose concentrations were increased in both diabetic control and Forskolin-treated groups compared to normal controls, but due to down-regulation of glucose transporter protein 1 expression, the Forskolin-treated group was only about 68.06% of the diabetic control group. ICAM-1 and TNF-α expression was up-regulated in the Forskolin-treated and diabetic control groups compared to the normal control group, but the expression levels of these two inflammatory factors in the Forskolin-treated group were 68.75% and 75.37% of those in the diabetic control group, respectively. [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 Coleonol, Colforsin
Molecular Weight 410.5
Formula C22H34O7
CAS No. 66575-29-9

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 30 mg/mL (73 mM)

Ethanol: 15 mg/mL (36.5 mM)

TargetMolReferences and Literature

1. Park KH, et al. Modulation of PC12 cell viability by forskolin-induced cyclic AMP levels through ERK and JNK pathways: an implication for L-DOPA-induced cytotoxicity in nigrostriatal dopamine neurons. Toxicol Sci. 2012 Jul;128(1):247-57. 2. Follin-Arbelet V, et al. The natural compound forskolin synergizes with dexamethasone to induce cell death in myeloma cells via BIM. Sci Rep. 2015 Aug 26;5:13001. 3. 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. 4. Follin-Arbelet V, et al. Cyclic AMP induces apoptosis in multiple myeloma cells and inhibits tumor development in a mouse myeloma model. BMC Cancer. 2011 Jul 18;11:301. 5. You ZP, et al. Forskolin attenuates retinal inflammation in diabetic mice. Mol Med Rep. 2018 Feb;17(2):2321-2326. 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.

TargetMolCitations

1. Li J, Bai Y, Liu Y, et al.Transcriptome-based chemical screens identify CDK8 as a common barrier in multiple cell reprogramming systems.Cell Reports.2023, 42(6). 2. Han L, Song B, Zhang P, et al.PC3T: a signature-driven predictor of chemical compounds for cellular transition.Communications Biology.2023, 6(1): 989. 3. Chen S, Zhou X, Li W, et al.Development of a novel peptide targeting GPR81 to suppress adipocyte-mediated tumor progression.Biochemical Pharmacology.2023: 115800. 4. Ma X, Lu Y, Zhou Z, Human expandable pancreatic progenitor–derived β cells ameliorate diabetes. Science Advances. 2022, 8(8): eabk1826. 5. Fu J, Jiang L, Yu B, et al. Generation of a Human iPSC Line CIBi010-A with a Reporter for ASGR1 Using CRISPR/Cas9. Stem Cell Research. 2022: 102800 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. 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. 8. Wu L, Dong A, Dong L, et al. PARIS, an optogenetic method for functionally mapping gap junctions. ELife. 2019 Jan 14;8. pii: e43366 9. 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 10. 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.
11. Zhang X, Ke P X, Yuan X, et al. Forskolin Protected against Streptozotocin-Induced Diabetic Cardiomyopathy via Inhibition of Oxidative Stress and Cardiac Fibrosis in Mice. BioMed Research International. 2021, 2021 12. 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 13. 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 14. 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 15. 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 16. Hu Z, Lu Y, Cao J, et al.N-acetyltransferase NAT10 controls cell fates via connecting mRNA cytidine acetylation to chromatin signaling.Science Advances.2024, 10(2): eadh9871. 17. Zhao X, Cai X, Zhu H, et al.27-Hydroxycholesterol inhibits trophoblast fusion during placenta development by activating PI3K/AKT/mTOR signaling pathway.Archives of Toxicology.2024: 1-15. 18. Mendonça L S, Henriques D, Fernandes V, et al.Graft-derived neurons and bystander effects are maintained for six months after human iPSC-derived NESC transplantation in mice’s cerebella.Scientific Reports.2024, 14(1): 3236. 19. Dang Q, Zhu Y, Zhang Y, et al.Nuclear Binding Protein 2/Nesfatin-1 Affects Trophoblast Cell Fusion during Placental Development via the EGFR-PLCG1-CAMK4 Pathway.International Journal of Molecular Sciences.2024, 25(3): 1925.
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Keywords

Forskolin 66575-29-9 Autophagy Metabolism Neuroscience FXR Adenylyl cyclase AChR notropic pregnane Inhibitor exosome cancer antihypertensive antiaggregatory X receptor prostate NR1H4 Adenylate Cyclase PXR Coleonol Colforsin cAMP inhibit inhibitor

 

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