Forskolin (Colforsin)

別名：HL 362, Coleonol

製品コード：S2449 純度：99.06%

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、PXR と FXR 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。

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
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
100mg	JPY 85500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（154）

製品安全説明書

現在のバッチを見る：純度： 99.06%

99.06

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.

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

関連ターゲット	AC EPAC1 EPAC2 PACAP receptor	もっと見る
関連製品	SQ22536 ESI-09 PACAP 1-38 Bithionol PACAP 6-38 acetate HJC0350	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I GPCR Compound Library	もっと見る

シグナル伝達経路

cAMP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

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 (G_s)–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
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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	--

参考
[1] Insel PA, et al. Cell Mol Neurobiol, 2003, 23(3), 305-314. [2] Wagh VD, et al. J Postgrad Med, 2012, 58(3), 199-202. [3] Liang C, et al. Nucleic Acids Res. 2022 Apr 8;50(6):3323-3347. [4] El-Agroudy NN, et al. Br J Pharmacol. 2016 Nov;173(22):3248-3260. + 展開

参考

[4] El-Agroudy NN, et al. Br J Pharmacol. 2016 Nov;173(22):3248-3260.

+ 展開

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	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管		溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 40 mg/mL ( (97.44 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 : 20 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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):