Forskolin (Colforsin)

別名:HL 362, Coleonol

コルホルチン (Forskolin (Colforsin)) は、広範な細胞腫における真核生物のアデニル酸シクラーゼ (adenylate cyclase, AC) の遍在する活性化因子であり、細胞生理学の研究において cAMP のレベルを上げるために一般的に使用されています。ホルスコリン (Forskolin) は、PXRFXR も活性化します。 ホルスコリンはオートファジー (autophagy) を刺激します。

Forskolin (Colforsin)化学構造

CAS No. 66575-29-9

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 40500 国内在庫あり
JPY 55500 国内在庫あり
JPY 85500 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(145)

製品安全説明書

現在のバッチを見る: 純度: 99.20%
99.20

Forskolin (Colforsin)と併用されることが多い化合物

SQ22536


SQ22536 inhibits the elevation of cAMP content and adenylyl cyclase activity caused by forskolin.

Gao Y, et al. Eur J Pharmacol. 2001 Apr 20;418(1-2):111-6.

VPA (Valproic acid)


VPA significantly decreases PKA-dependent enhancement of mossy fiber transmission, following activation of adenylyl cyclase with forskolin.

Chang P, et al. Epilepsia. 2010 Aug;51(8):1533-42.

RepSox (E-616452)


RepSox and Forskolin along with other chemical cocktails are used together in reprogramming and chemical induction of iPSCs

Xie X, et al. Curr Opin Genet Dev. 2017 Oct;46:104-113.

TTNPB


TTNPB and Forskolin along with other small molecules can convert human urine cells into neurons directly, without introducing the transcription factors or miRNAs.

Xu G, et al. Sci Rep. 2019 Nov 13;9(1):16707.

EPZ004777


EPZ004777 and Forskolin are used in combination with other small molecules as cocktail in the medium for direct reprogramming of mouse fibroblasts into ciNCCs and ciCECs

Pan SH, et al. Sci Adv. 2021 Jun 4;7(23):eabg5749.

Forskolin (Colforsin)関連製品

シグナル伝達経路

cAMP阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
SH-SY5Y  Function Assay 10 μM 1 h  increases LUC activity 25597433
SH-SY5Y  Function Assay 10 μM 1 h  increases AGC1 mRNA level 25597433
hADSCs Function Assay 5 µM 30 min increases cAMP levels 25591908
HEK293  Function Assay 5 µM 30 min increases cAMP levels 25591908
3T3-L1 Function Assay 2.5/5 μM 24 h  significantly decreases ATGL protein expression at all doses tested 25590597
OCI-Ly1  Function Assay 40 μM 1 h  induces the increment of cAMP concentrations 25576220
OCI-Ly18  Function Assay 40 μM 1 h  induces the increment of cAMP concentrations 25576220
BeWo Function Assay 20 µM 48 h increases the differentiation of BeWo cells 25566740
BeWo Function Assay 20 µM 48 h increases the adhesion of THP-1 monocytes 25566740
LNCaP  Function Assay 10 μM 12 h  induces a dramatic increase of CREB1 activity 25548099
ThGCs  Function Assay 10 μM 4 h augments HIF1A levels that were stimulated by CoCl2 25433027
ThGCs  Function Assay 10 μM 4 h increases CoCl2-induced EDN2 gene expression 25433027
ThGCs  Function Assay 10 μM 3 h inhibits the effect of H2O2 on EDN2 mRNA 25433027
RBMECs Function Assay 0.05/0.5/5 μM 0.25 h increases cAMP concentration 25416651
RBMECs Function Assay 5 μM 1 h blocks the activation of RhoA/ROCK induced by EMAP-II 25416651
RBMECs Function Assay 5 μM 1 h prevents the EMAP-II-induced TEER value decrease 25416651
RBMECs Function Assay 5 μM 1 h prevents the increase in HRP flux across the BTB induced by EMAP-II 25416651
RBMECs Function Assay 5 μM 1 h inhibits the decreased of amount of ZO-1 in MFs induced by EMAP-II 25416651
RBMECs Function Assay 5 μM 1 h reverses the changes in ZO-1 distribution seen with EMAP-II treatment 25416651
RBMECs Function Assay 5 μM 1 h blocks the EMAP-II-induced change in MLC phosphorylation 25416651
RBMECs Function Assay 5 μM 1 h blocks the actin cytoskeleton rearrangement seen with EMAP-II treatment  25416651
Primary bovine chondrocytes Growth Inhibition Assay 5μM 48 h reverses the inhibitory effect of celecoxib on proliferation in growth plate chondrocytes 25406016
EM1  Function Assay 15 μM 48 h reduces the expression of LIF or PTGS2 in CALR- or EPAC2-silenced EM1 cells  25378661
BeWo  Function Assay 20 µM 48 h  increases the beta-hCG release 25362260
BeWo  Function Assay 20 µM 48 h  downregulates the level of TMEMF16 25362260
BeWo  Function Assay 20 µM 48 h  downregulates the level of GCM-1 25362260
granulosa cells Function Assay 10 μM 12/24 h increases the levels of RGS2 mRNA 25339105
granulosa cells Function Assay 10 μM 12/24 h increases the levels of reporter activity for the longest fragment (−854/+18RGS2.LUC) 25339105
granulosa cells Function Assay 10 μM 24 h increases the intensity of DNA/protein complex 25339105
granulosa cells Function Assay 10 μM 24 h increases the levels of RGS2 promoter activity 25339105
SK-N-AS  Cell Viability Assay 10 μM  24/48 h enhances time-dependently cellular viability  25266063
SK-N-AS  Function Assay 10 μM  24 h increases the cAMP levels  25266063
SK-N-AS  Function Assay 10 μM  24 h increases the expression of cyclin D1 25266063
SK-N-AS  Function Assay 10 μM  30 min induces phosphorylation of β-catenin (ser675), p-GSK3β (ser9) and concomitant higher levels of active, unphosphorylated, β-catenin 25266063
SK-N-AS  Function Assay 10 μM  10/30/60 min increases levels of p-β-catenin (ser675) and induces accumulation of p-β-catenin (ser675) in (peri)nuclear regions 25266063
SK-N-SH Cell Viability Assay 10 μM  48 h enhances SK-N-SH neuroblastoma cell viability 25266063
HEK‐CFTR Function Assay 2–50 μM 0-12 min induces a dose‐dependent iodide efflux  25263207
L6 Function Assay 40 µM 24 h inhibits DMH1-induced Akt activation 25247550
MIN6  Function Assay 10 μM  3 h increases D3 mRNA expression 25241124
BeWo  Function Assay 20 µM 48 h induces cell fusion 25184477
THP-1  Function Assay 1/10 μM 2 h suppresses MCP-1 production  25154882
Huh-7 Function Assay 0-20 μM 2 h  results in a dose-dependent increase in c-Myc expression at the protein and mRNA levels 25109834
C6 Function Assay 10 μM  20 min increases cAMP accumulation 25069417
SW480 Function Assay 40 μM 48 h activates PP2A 24997451
HT-29  Function Assay 40 μM 48 h activates PP2A 24997451
SW480 Growth Inhibition Assay 40 μM 0-72 h inhibits cell growth time dependently 24997451
HT-29  Growth Inhibition Assay 40 μM 0-72 h inhibits cell growth time dependently 24997451
SW480 Function Assay 40 μM 7 d reduces colonosphere formation capability  24997451
HT-29  Function Assay 40 μM 7 d reduces colonosphere formation capability  24997451
SW480 Apoptosis Assay 40 μM 48 h induces an activation of caspase 3/7 24997451
HT-29  Apoptosis Assay 40 μM 48 h induces an activation of caspase 3/7 24997451
SW480 Apoptosis Assay 40 μM 48 h induces changes in the phosphorylation status of PP2A targets 24997451
HT-29  Apoptosis Assay 40 μM 48 h induces changes in the phosphorylation status of PP2A targets 24997451
UACC-647  Function Assay 10 μM 15 min increases eEF2 phosphorylation levels  25703025
UACC-647  Function Assay 10 μM 15 min inhibits ERK phosphorylation 25703025
SC Function Assay 0.5 μM 72 h increases both Krox-20 and O1 expression in axon-related SCs but only Krox-20  25705874
SC Function Assay 0.5 μM 24 h mimicks the effect of cAMP analogs on O1 and MBP expression 25705874
oocytes Function Assay 5 μM 24 h attenuates rh-insulin action on oocyte GVBD significantly  25707854
BeWo Function Assay 10 μM  72 h mediates BeWo cell differentiation 25713425
GH3 Function Assay 1 μM 6-h induces PRL and Bmal1, but not Clock, mRNA expression 25727018
GH3 Function Assay 1 μM 6-h attenuates the correlation between PRL and Bmal1 expression 25727018
PC12 Function Assay 25 μM 48 h activates cAMP 25769305
BAECs Function Assay 25 μM 24 h enhances the activation of PPARα by 5 μM resveratrol, T4HS, or 4-PAP 25798826
GLUTag  Function Assay 10 µM 4 h increases the pCREB levels with the IBMX 25832631
GLUTag  Function Assay 10 µM 0/2/4 h stimulates GLP-1 secretion cotreated with IBMX 25832631
PBMC Function Assay 50 μM 24 h  inhibits the increased secretion of TNF induced by the DPE 25866079
H295R  Function Assay 10 μM 48 h increases steroid metabolites in the androgen, mineralo- and glucocorticoid pathways 25869556
3T3-L1 preadipocytes Function Assay 10 μM  12 h induces CREB phosphorylation and C/EBPβ expression 25928058
PCCL3 Function Assay 10 µM 24 h enhances DuOx2 promoter transcription activity ​ 25960956
PC-3 Cell Viability Assay 40 µM 24/48/72 h decreases cell viability time dependently 26023836
PC-3 Function Assay 40 µM 2 h leads to PP2A activation 26023836
SH-SY5Y Function Assay 30 μM 30 min significantly increases the activation of PKA 26025137
EndoC-βH1 Function Assay 5 μM 1 h leads to a strong cAMP increase 26028562
EndoC-βH1 Function Assay 5 μM 1 h potentiates glucose-induced insulin secretion in the presence of glucose 26028562
RBMECs Function Assay 5 μM 1 h inhibits EMAP-II-induced inactivation of Rap1  26044663
AML-12  Function Assay 20 μM 3 h induces the dephosphorylation of CRTC2  26048985
AML-12  Function Assay 20 μM 3 h up-regulates Pgc1a, Pepck, and G6pc mRNA levels 26048985
AML-12  Function Assay 20 μM 1-8 h increases glucose production 26048985
AML-12  Function Assay 20 μM 3 h upregulates the phosphorylation levels at Thr-411 and Ser-493 26048985
Caco-2  Function Assay 0.1/1/10 μM 24 h increases MRP2 protein level 26049102
Caco-2  Function Assay 0.1/1/10 μM 20 min induces a dose-dependent increase in intracellular cAMP levels 26049102
bovine oocytes Function Assay 100 μM 12 h inhibits the effect of NPPA and/or NPPC to stimulate resumption of meiosis 26051611
BeWo  Function Assay 25 μM 24/48/72 h leads to an increase in the expression of other fusion markers 26053549
Spinal cords  Function Assay 1 μM 30 min stimulates cAMP levels 26126926
MDCK  Function Assay 10 µM 24 h inhibits the increased expression of FN caused by TGF-β1 26202352
MDCK  Function Assay 10 µM 24 h upregulates the expression of TGF-β1 and CTGF  26202352
RPMI 8226 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
H929 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
U266 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
OPM-2 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
INA-6 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
RBMECs  Function Assay 5 μM 1 h blocks the Rac1 inactivation induced by EMAP-II 26358039
Mo-DCs Function Assay 50 μM 24 h promotes IL-23 production in the supernatant of zymosan stimulated Mo-DCs  26412948
HEK293 Function Assay 10 μM 6 h increases phosphorylation of overexpressed KLHL3 at S433 26435498
epithelial cells Function assay 1 uM 4, 6, and 8 days 19966789
HEK293 Function assay 10 uM 16 hrs 26435512
ventricular cardiomyocytes  Function Assay 0.01-10 μM increases cAMP accumulation 25203113
ventricular cardiomyocytes  Function Assay 0.01-10 μM evokes an inotropic response 120±15% above basal with an EC50 of 2.2 µM 25203113
SCG Function Assay 100 μM  reduces the excitability of SCG neurons 25962132
HEK-293 Function Assay 35 μM  induces a conspicuous “inactivation” of the Kv2.1 current 25962132
SCG Function Assay 20 μM  reversibly suppresses IKV with a IC50 of 24.4 μM 25962132
HEK293T Function assay 10 uM 24387325
ASK Function assay 1 hr 2849641
HepG2 (DPX-2) Function assay 24 hrs 20966043
HepG2 Function assay 24 hrs 20966043
HepG2 (DPX-2) Function assay 24 hrs 20966043
MCF7 Cytotoxicity assay 48 hrs 28838692
HEK293 Function assay 30 mins 30006176
UACC-647  Function Assay leads to a rise in cAMP levels (EC50 = 20.39 μM) 25703025
Vero E6 Antiviral assay 17663539
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生物活性

製品説明 コルホルチン (Forskolin (Colforsin)) は、広範な細胞腫における真核生物のアデニル酸シクラーゼ (adenylate cyclase, AC) の遍在する活性化因子であり、細胞生理学の研究において cAMP のレベルを上げるために一般的に使用されています。ホルスコリン (Forskolin) は、PXRFXR も活性化します。 ホルスコリンはオートファジー (autophagy) を刺激します。
Targets
Adenylyl cyclase (AC) [1]
(A wide variety of cell types)
In Vitro
In vitro

Forskolin increases cAMP levels in preparations of membranes, cells, or tissues. Forskolin not only activates AC but also interacts with certain other proteins, including glucose transporters and ion channels. Forskolin is able to promote activation of nine different transmembrane iso-forms of AC, albeit with somewhat less efficacy for AC9, which could be used to provides a means to identify and quantify high-affinity binding sites, i.e., G-proteins (Gs)–AC complexes. Activation of s by GPCRs contributes to Forskolin-stimulated cAMP generation in cells because of s-Forskolin potentiation of AC activity. [1] Forskolin stimulates adenylate cyclase activity without interacting with cell surface receptors. Forskolin's potentiation of cAMP in turn inhibits basophil and mast cell degranulation and histamine release, lowers blood pressure and intraocular pressure, inhibits platelet aggregation, promotes vasodilation, bronchodilation, and thyroid hormone secretion, and stimulates lipolysis in fat cells. Forskolin inhibits the binding of platelet-activating factor (PAF), independently of cAMP formation, which may be a result of Forskolin's direct effect on PAF or via interference with PAF binding to receptor sites. Forskolin also appears to have an effect on several membrane transport proteins, and inhibits glucose transport in erythrocytes, adipocytes, platelets, and other cells. Forskolin is used to treat with glaucoma. [2]

細胞実験 細胞株 hMPCs or cynMPCs
濃度 20 μM
反応時間 2 h
実験の流れ

Cells were treated with 20 μM forskolin (S2449, Selleck) for 2 h for synchronization.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot cleaved caspase-3 / caspase-3 cleaved caspase-9 / caspase-9 β-catenin c-myc / Cyclin D1 pS6K1 / S6K1 / pCREB / CREB p-JNK / JNK / P-p38 / p38 30863177
Immunofluorescence 5hmC Fe(II) CYP17A1 / CYP21A2 29239726
Growth inhibition assay Cell viability 30863177
In Vivo
In Vivo

Colforsin (Forskolin, HL 362, Coleonol) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP. It also activates PXR and FXR activity and stimulates autophagy.[4]

動物実験 動物モデル Male Sprague-Dawley rats
投与量 10 mg/kg
投与経路 i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04254705 Withdrawn
Cystic Fibrosis
Universitaire Ziekenhuizen KU Leuven|Vertex Pharmaceuticals Incorporated|KU Leuven|University of Lisbon
March 1 2020 Not Applicable
NCT02807415 Completed
Cystic Fibrosis
Hannover Medical School|Heidelberg University|University of Giessen
June 1 2016 --
NCT02586883 Completed
Idiopathic Dilation of the Bronchi
Assistance Publique - Hôpitaux de Paris
March 29 2016 Not Applicable
NCT03652090 Completed
Cystic Fibrosis
Institut National de la Santé Et de la Recherche Médicale France|ABCF2
September 1 2010 --

化学情報

分子量 410.5 化学式

C22H34O7

CAS No. 66575-29-9 SDF Download Forskolin (Colforsin) SDFをダウンロードする
Smiles CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O
保管 3 years -20°C(in the dark) powder
1 year -80°C(in the dark) in solvent

In vitro
Batch:

DMSO : 82 mg/mL ( (199.75 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 82 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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