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Purity: ≥98%
Forskolin (HL-362; L-75-1362B; NSC-357088; NSC-375489; Coleonol; Colforsin), a naturally occurring and cell-permeable diterpene extracted from the Indian Coleus plant (C. forskohlii), is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types. It can improve the in vivo production of bone by human mesenchymal stromal cells. In the study and investigation of cell physiology, forskolin is frequently used to increase cAMP levels. With an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase, respectively, it functions as a strong activator of adenylate cyclase. In the rat myometrium, forskolin regulates the production of cyclic AMP. Interactions with isoproterenol and prostaglandins E2 and I2.
| Targets |
Adenylyl cyclase ( IC50 = 41 nM ); Adenylyl cyclase ( EC50 = 0.5 μM )
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| ln Vitro |
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| ln Vivo |
The Forskolin (Fsk)-treated Mrp4-/- mice shows 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 shows a significant increase in the unvascularized retinal area[3]. The average blood glucose in the healthy rat group is 102.12±1.94 mg/dL, 101.25±3.56 for control group and 103±2.08 in forskolin group. The data shows that glucose levels at the end of the study are lower in forskolin group, with a significant difference according to the statistical tests applied (p=0.03)[6].
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| Enzyme Assay |
In Vitro Kinase Assays[5]
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 (described above). Jak3-bound PAS beads were washed three times in cold lysis buffer (described above) 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-nitrophenylphosphate, 0.1% Triton X-100) and one time in kinase wash buffer (described above). 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. |
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| Cell Assay |
In 96-well plates, 5×104 cells of either MT-2 or Quiescent Kit 225 are seeded into each well. Afterwards, cells are pretreated for one hour at concentrations of 1, 5, 10, 25, 50, and 100 μM of forskolin or 1% DMSO (vehicle). Following 20 hours of culture at 37°C and IL-2 stimulation, the cells are harvested. A 20-hour treatment of 1% DMSO is given to control cells. [3H]thymidine is pulsed into the cells at a concentration of 0.5 μCi/200 μL during the last 4 hours of incubation. Using liquid scintillation counting, cells are collected onto fiberglass filters for analysis.
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| Animal Protocol |
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| References |
[1]. Cell Mol Neurobiol. 2003 Jun;23(3):305-14. [2]. J Postgrad Med. 2012 Jul-Sep;58(3):199-202. [3]. Nucleic Acids Res. 2022 Apr 8;50(6):3323-3347. [4]. Br J Pharmacol. 2016 Nov;173(22):3248-3260. [5]. J Biol Chem. 2013 Mar 8;288(10):7137-46. doi: 10.1074/jbc.M112.408765. Epub 2013 Jan 2. |
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| Additional Infomation |
Forskolin is a labdane diterpenoid isolated from the Indian Coleus plant. It has a role as a plant metabolite, an anti-HIV agent, a protein kinase A agonist, an adenylate cyclase agonist, an antihypertensive agent and a platelet aggregation inhibitor. It is a labdane diterpenoid, an acetate ester, an organic heterotricyclic compound, a triol, a cyclic ketone and a tertiary alpha-hydroxy ketone.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant Coleus forskohlii. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland. Forskolin is a natural product found in Plectranthus, Apis cerana, and Plectranthus barbatus with data available. |
| Molecular Formula |
C22H34O7
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| Molecular Weight |
410.5
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| Exact Mass |
410.23
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| Elemental Analysis |
C, 64.37; H, 8.35; O, 27.28
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| CAS # |
66575-29-9
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| Related CAS # |
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| PubChem CID |
47936
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
519.9±50.0 °C at 760 mmHg
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| Flash Point |
171.8±23.6 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.552
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| LogP |
3.4
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| tPSA |
113.29
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| SMILES |
CC(=O)O[C@H]1[C@H]([C@@H]2[C@]([C@H](CCC2(C)C)O)([C@@]3([C@@]1(O[C@@](CC3=O)(C)C=C)C)O)C)O
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| InChi Key |
OHCQJHSOBUTRHG-KGGHGJDLSA-N
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| InChi Code |
InChI=1S/C22H34O7/c1-8-19(5)11-14(25)22(27)20(6)13(24)9-10-18(3,4)16(20)15(26)17(28-12(2)23)21(22,7)29-19/h8,13,15-17,24,26-27H,1,9-11H2,2-7H3/t13-,15-,16-,17-,19-,20-,21+,22-/m0/s1
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| Chemical Name |
[(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-ethenyl-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-5,6,6a,8,9,10-hexahydro-2H-benzo[f]chromen-5-yl] acetate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4361 mL | 12.1803 mL | 24.3605 mL | |
| 5 mM | 0.4872 mL | 2.4361 mL | 4.8721 mL | |
| 10 mM | 0.2436 mL | 1.2180 mL | 2.4361 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01254006 | Completed | Drug: forskolin, rutin and vitamins B1 and B2 |
Glaucoma | University of Roma La Sapienza | N/A | Not Applicable |
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