Forskolin

• CAT Number: I004502
• CAS Number: 66575-29-9
• Molecular Formula: C22H34O7
• Molecular Weight: 410.5
• Purity: ≥95%
• Target: Adenylate cyclase
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder
• IC50: 0.5 uM (EC50)
• InChIKey: OHCQJHSOBUTRHG-KGGHGJDLSA-N

Forskolin(Colforsin) is a labdane diterpenoid with antihypertensive, positive inotropic, platelet aggregation inhibitory and adenylate cyclase activating properties.IC50 Value: 0.5 uM (EC50)Target: Adenylate cyclasein vitro: Forskolin (10 microM) rapidly increased cAMP levels in bovine thyroid slices both in the absence and presence of a phosphodiesterase inhibitor. The effect of TSH (50 mU/ml) on cAMP levels was additive or greater than additive to that of forskolin [1]. Fsk treatment of MT-2 and Kit 225 T-cells inhibited IL-2-induced Stat5a/b tyrosine and serine phosphorylation, nuclear translocation, and DNA binding activity. Fsk treatment also uncoupled IL-2 induced association of the IL-2Rβ and γc chain, consequently blocking Jak3 activation [2].in vivo: Low concentrations of forskolin (0.1-1.0 microM), which significantly elevated cyclic AMP levels, did not increase lipolysis, whereas similar increases in cyclic AMP levels due to isoproterenol elevated lipolysis. Forskolin did not inhibit the activation of triacylglycerol lipase by cyclic AMP-dependent protein kinase or the subsequent hydrolysis of triacylglycerol [3]. Colforsin-induced vasodilation was impaired in both +E and -E arteries from PH rats compared with their respective controls. Endothelial removal did not influence colforsin-induced vasodilation in the arteries from control rats, but attenuated it in arteries from PH rats [4].Clinical trial: N/A

Reference

1:Adenyl cyclase activator forskolin protects against Huntington/’s disease-like neurodegenerative disorders. Mehan S, Parveen S, Kalra S.Neural Regen Res. 2017 Feb;12(2):290-300. doi: 10.4103/1673-5374.200812. PMID: 28400813 Free PMC Article2:Total biosynthesis of the cyclic AMP booster forskolin from Coleus forskohlii. Pateraki I, Andersen-Ranberg J, Jensen NB, Wubshet SG, Heskes AM, Forman V, Hallström B, Hamberger B, Motawia MS, Olsen CE, Staerk D, Hansen J, Møller BL, Hamberger B.Elife. 2017 Mar 14;6. pii: e23001. doi: 10.7554/eLife.23001. PMID: 28290983 Free PMC Article3:Forskolin-induced Swelling in Intestinal Organoids: An In Vitro Assay for Assessing Drug Response in Cystic Fibrosis Patients. Boj SF, Vonk AM, Statia M, Su J, Vries RR, Beekman JM, Clevers H.J Vis Exp. 2017 Feb 11;(120). doi: 10.3791/55159. PMID: 28287550 4:Evening primrose oil or forskolin ameliorates celecoxib-enhanced upregulation of tissue factor expression in mice subjected to lipopolysaccharide-induced endotoxemia. Mosaad SM, Zaitone SA, Ahmed AA, Abo-Elmatty DM, El-Baz AA, Moustafa YM.Naunyn Schmiedebergs Arch Pharmacol. 2017 May;390(5):483-492. doi: 10.1007/s00210-017-1342-y. Epub 2017 Jan 26. PMID: 28124089 5:Forskolin Induces Hyperphosphorylation of Tau Accompanied by Cell Cycle Reactivation in Primary Hippocampal Neurons. Wang HH, Li Y, Li A, Yan F, Li ZL, Liu ZY, Zhang L, Zhang J, Dong WR, Zhang L.Mol Neurobiol. 2016 Dec 19. doi: 10.1007/s12035-016-0348-7. [Epub ahead of print] PMID: 27995573 6:Adenylyl cyclase 3/adenylyl cyclase-associated protein 1 (CAP1) complex mediates the anti-migratory effect of forskolin in pancreatic cancer cells. Quinn SN, Graves SH, Dains-McGahee C, Friedman EM, Hassan H, Witkowski P, Sabbatini ME.Mol Carcinog. 2017 Apr;56(4):1344-1360. doi: 10.1002/mc.22598. Epub 2016 Dec 29. PMID: 27891679 7:Forskolin Inhibits Lipopolysaccharide-Induced Modulation of MCP-1 and GPR120 in 3T3-L1 Adipocytes through an Inhibition of NFκB. Chiadak JD, Arsenijevic T, Verstrepen K, Gregoire F, Bolaky N, Delforge V, Flamand V, Perret J, Delporte C.Mediators Inflamm. 2016;2016:1431789. Epub 2016 Nov 2. PMID: 27881903 Free PMC Article8:Enhancement of UV-induced nucleotide excision repair activity upon forskolin treatment is cell growth-dependent. Lee JM, Park JM, Kang TH.BMB Rep. 2016 Oct;49(10):566-571. PMID: 27470212 Free PMC Article9:Sensitivity of imatinib-resistant T315I BCR-ABL CML to a synergistic combination of ponatinib and forskolin treatment. Oaxaca DM, Yang-Reid SA, Ross JA, Rodriguez G, Staniswalis JG, Kirken RA.Tumour Biol. 2016 Sep;37(9):12643-12654. Epub 2016 Jul 21. PMID: 27444277 Free PMC Article10:Forskolin, a hedgehog signalling inhibitor, attenuates carbon tetrachloride-induced liver fibrosis in rats. El-Agroudy NN, El-Naga RN, El-Razeq RA, El-Demerdash E.Br J Pharmacol. 2016 Nov;173(22):3248-3260. doi: 10.1111/bph.13611. Epub 2016 Oct 4. PMID: 27590029