Forskolin  (Synonyms: Coleonol; Colforsin; HL 362)

Forskolin (Coleonol) (GMP) 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 (GMP) is also an inducer of intracellular cAMP formation^[2]. Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR^[3]. Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy^[4][5].

Forskolin (Coleonol) (GMP) is also a potent exosome biogenesis and/or secretion activator in prostate cancer (PC) cells^[8].
Forskolin (GMP) is a naturally occurring diterpene isolated from Coleus forskholii, directly activates adenylyl cyclase (AC) through its catalytic subunit to increase intracellular levels of cyclic adenosine monophosphate (cAMP)^[1].
Forskolin (GMP) affects the proliferation of the human T-cell lines such as Kit 225 and MT-2. Forskolin (GMP) treatment inhibits the proliferation of both Kit 225 and MT-2 cells in a dose-dependent manner with an IC₅₀ equal to ~5 μM Forskolin (GMP). Forskolin (GMP) treatment (10-100 μM) increases cAMPi levels ~5- to 20-fold above basal levels, which reache maximum levels between 50-100 μM Forskolin (GMP)^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

The Forskolin (Coleonol) (GMP)-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^[2].
The average blood glucose in the healthy rat group is 102.12 mg/dL, 101.25 for control group and 103 in Forskolin (GMP) group. The data shows that glucose levels at the end of the study are lower in Forskolin (GMP) group, with a significant difference according to the statistical tests applied^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

410.50

C₂₂H₃₄O₇

66575-29-9

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [3]. Mayati A, et al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]