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. Forskolin (GMP) is also an inducer of intracellular cAMP formation. Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy.
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- CAS No.: 66575-29-9
- 화학식: C22H34O7
- 분자량:410.50
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | IC50 |
>100 μM
Compound: 1
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Antiproliferative activity against human BT474 cells after 48 hrs by Alamar blue assay
Antiproliferative activity against human BT474 cells after 48 hrs by Alamar blue assay
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[PMID: 28838692] |
| HEK293 | EC50 |
0.0937 μM
Compound: FSK
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Agonist activity at recombinant human AC8 expressed in human HEK293 cells assessed as fold increase in cAMP level by LANCE Ultra cAMP Detection kit method
Agonist activity at recombinant human AC8 expressed in human HEK293 cells assessed as fold increase in cAMP level by LANCE Ultra cAMP Detection kit method
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[PMID: 31776060] |
| Hepatocyte | EC50 |
0.7 μM
Compound: Colforsin
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Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4
Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4
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[PMID: 20966043] |
| HepG2 | EC50 |
2.7 μM
Compound: Colforsin
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
7.1 μM
Compound: Colforsin
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Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
7.9 μM
Compound: Colforsin
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Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| MCF7 | IC50 |
63.3 μM
Compound: 1
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Antiproliferative activity against human MCF7 cells after 48 hrs by Alamar blue assay
Antiproliferative activity against human MCF7 cells after 48 hrs by Alamar blue assay
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[PMID: 28838692] |
| NIH-3T3-G185 | IC50 |
188.2 μM
Compound: Forskolin
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TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
80.2 μM
Compound: Forskolin
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TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| Vero | CC50 |
674 μM
Compound: 10
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Cytotoxicity against Vero E6 cells by MTT assay
Cytotoxicity against Vero E6 cells by MTT assay
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[PMID: 17663539] |
| Vero | EC50 |
7.5 μM
Compound: 10
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Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA
Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA
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[PMID: 17663539] |
| Vero C1008 | IC50 |
>2.0 × 105M
Compound: COVC-1212934635
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
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10.6019/CHEMBL4651402 |
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 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.
Chemical Information
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CAS No. 66575-29-9
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분자량 410.50
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화학식 C22H34O7
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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
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Synonyms
Coleonol (GMP); Colforsin (GMP); HL 362 (GMP)
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Forskolin (GMP) Related Classifications
HY-15371G Related Classifications
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