Forskolin

Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase[1]. Forskolin is also an inducer of intracellular cAMP formation[2]. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR[3]. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy[4][5].

Product Specifications

CAS Number

[66575-29-9]

Product Name Alternative

Coleonol; Colforsin; HL 362

UNSPSC

12352005

Hazard Statement

H312

Target

Adenylate Cyclase; Autophagy; FXR; Organoid; PKC

Type

Natural Products

Related Pathways

Autophagy; Epigenetics; GPCR/G Protein; Metabolic Enzyme/Protease; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-programmed cell death

Field of Research

Cancer; Endocrinology; Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Forskolin.html

Purity

99.94

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1[C@@]2(O)[C@]([C@@H](OC(C)=O)[C@@H](O)[C@@]3([H])C(C)(C)CC[C@H](O)[C@@]32C)(C)O[C@@](C)(C=C)C1

Molecular Formula

C22H34O7

Molecular Weight

410.50

Precautions

H312

References & Citations

[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]Matsumiya W, et al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53 (13) :8029-35. |[3]Mayati A, et al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8 (1) :16115.|[4]Awad JA, 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 Mar 10;258 (5) :2960-5.|[5]Seamon KB, et al. Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives. J Med Chem. 1983 Mar;26 (3) :436-9.|[6]Ríos-Silva M, et al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimental diabetes. Int J Med Sci. 2014 Mar 11;11 (5) :448-52.|[7]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.|[8] Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8 (1) :8161.