B1421-100mg | Forskolin [66575-29-9] Clinisciences

Forskolin is a cell-permeable activator of adenylyl cyclase [1].

Adenylate cyclase is an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to 3',5'-cyclic AMP (cAMP) and pyrophosphate.

Forskolin is a cell-permeable activator of adenylyl cyclase. In rat cerebral cortical membranes, forskolin reversibly and rapidly activated adenylate cyclase with EC50 value of 5-10 μM. GTP and GDP increased the responses to forskolin. In rat cerebral cortical slices, forskolin rapidly increased cAMP by 35-fold with IC50 values of 25 μM [1]. Forskolin inhibited the inactivation of adenylate cyclases induced by N-ethylmaleimide with Kd values of 7.6 and 6.3 μM for the platelet and brain adenylate cyclases, respectively. Also, forskolin protected adenylate cyclases against thermal inactivation. Forskolin activated the platelet adenylate cyclase with IC50 and Kd values of 3-10 μM and 9-11 μM, respectively [2]. In pig epidermal cells, forskolin activated epidermal adenylate cyclase with Ka value of 2-3×10-5 M and induced cAMP accumulations, which then inhibited mitotic in a dose-dependent way [3].

References:
[1]. Seamon KB, Padgett W, Daly JW. Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells. Proc Natl Acad Sci U S A, 1981, 78(6): 3363-3367.
[2]. Awad JA, Johnson RA, Jakobs KH, et al. Interactions of forskolin and adenylate cyclase. Effects on substrate kinetics and protection against inactivation by heat and N-ethylmaleimide. J Biol Chem, 1983, 258(5): 2960-2965.
[3]. Takeda J, Adachi K, Halprin KM, et al. Forskolin activates adenylate cyclase activity and inhibits mitosis in in vitro in pig epidermis. J Invest Dermatol, 1983, 81(3): 236-240.

1. Sneha Kesaraju, Yueying Li, et al. "Claudin-2 limits pancreatitis development through regulating tight junction-controlled pancreatic ductal transport." bioRxiv. September 11, 2023
2. Lina Xu, Guoliang Wang, et al. "A cocktail of small molecules maintains the stemness and differentiation potential of conjunctival epithelial cells." Ocul Surf. 2023 Aug 25;S1542-0124(23)00109-X. PMID: 37634570
3. Blackford SJI, Yu TTL, et al. "RGD density along with substrate stiffness regulate hPSC hepatocyte functionality through YAP signalling." Biomaterials 2023 Feb;293 PMID: 36640555
4. Lu Gan, Qiyong Li, et al. "Glucocorticoids rapidly promote YAP phosphorylation via the cAMP-PKA pathway to repress mouse cardiomyocyte proliferative potential." Mol Cell Endocrinol. 2022 Mar 10;548:111615. PMID: 35278645
5. Xiaoya An, Guoliang Wang, et al. "Novel cell culture paradigm prolongs mouse corneal epithelial cell proliferative activity in vitro and in vivo." Front Cell Dev Biol. 2021 Jun 30;9:675998. PMID: 34277619
6. Emilio J Vélez, Suraj Unniappan. "Nesfatin-1 and nesfatin-1-like peptide suppress growth hormone synthesis via the AC/PKA/CREB pathway in mammalian somatotrophs." Sci Rep. 2020 Oct 7;10(1):16686. PMID: 33028951
7. Liu DT, Hong WS, et al. "Upregulation of adamts9 by gonadotropin in preovulatory follicles of zebrafish." Mol Cell Endocrinol. 2019 Oct 2;499:110608. PMID: 31586455
8. Zhang H, Wen JJ, et al. "Forskolin reduces fat accumulation in Nile tilapia (Oreochromis niloticus) through stimulating lipolysis and beta-oxidation." Comp Biochem Physiol A Mol Integr Physiol. 2018 Dec 26;230:7-15. PMID: 30593869
9. Morel JD, Paatero AO, et al. "Proteomics reveals scope of mycolactone-mediated Sec61 blockade and distinctive stress signature." Mol Cell Proteomics. 2018 Jun 18. pii: mcp.RA118.000824. PMID: 29915147

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Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	410.5
Cas No.	66575-29-9
Formula	C₂₂H₃₄O₇
Solubility	insoluble in H2O; ≥13.43 mg/mL in EtOH; ≥20.53 mg/mL in DMSO
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
SDF	Download SDF
Canonical SMILES	C[C@]1([C@@H]([C@@H]2O)C(C)(C)CC[C@@H]1O)[C@]3(O)[C@]([C@H]2OC(C)=O)(C)O[C@@](C)(C=C)CC3=O
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Cell experiment [1, 2]:
Cell lines	Human mesenchymal stem cells
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	0.075-0.2 mM for 4 days or 7 days; or 10 μM
Applications	Forskolin concentration-dependently decreased human mesenchymal stem cells proliferation after 4 days. Moreover, Forskolin increased alkaline phosphatase (ALP) expression of human mesenchymal stem cells in a dose-dependent manner. Additionally, Forskolin (10 μM) significantly stimulated both vasopressin and oxytocin release from the rat hypothalamo-neurohypophysial (H-NH) system.
Animal experiment [1]:
Animal models	Particles were implanted in subcutaneous pockets of nude male mice model
Dosage form	0.10 or 0.15mM Forskolin
Applications	Treatment with 0.10 mM Forskolin enhanced bone formation by human mesenchymal stromal cells in vivo.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: 1. Doorn, J., Siddappa, R., van Blitterswijk, C. A. and de Boer, J. (2012) Forskolin enhances in vivo bone formation by human mesenchymal stromal cells. Tissue Eng Part A. 18, 558-567 2. Roszczyk, M. and Juszczak, M. (2014) Forskolin-stimulated vasopressin and oxytocin release from the rat hypothalamo-neurohypophysial system in vitro is inhibited by melatonin. Endokrynol Pol. 65, 125-131