Wortmannin (Synonyms: KY 12420)

Name: Wortmannin
Brand: GlpBio
SKU: GC12338
Availability: InStock
Rating: 5 (29 reviews)

رقم الكتالوجGC12338

وورتمانين هو مثبط مباشر قوي لخصائص PI3-كيناز المستمدة أصلاً من الفطريات (1،2).

Products are for research use only. Not for human use. We do not sell to patients.

Wortmannin التركيب الكيميائي

Cas No.: 19545-26-7

الحجم

السعر

المخزون

الكميّة

10mM (in 1mL DMSO)	80٫00	متوفر
5mg	61٫00	متوفر
10mg	88٫00	متوفر
20mg	142٫00	متوفر

Tel：(909) 407-4943 Email: sales@glpbio.com

مراجعات العميل

بناء على آراء العملاء.

Sample solution is provided at 25 µL, 10mM.

Product has been cited by 2 publications

Description Protocol Chemical Properties Product Documents Related Video

Product Documents

Quality Control & SDS

View current batch:

Purity: >99.50%

Protocol

Kinase experiment [1]:
Preparation Method	For studies of the kinetics of inhibition of PtdIns-3-kinase by wortmannin, bovine brain enzyme was incubated with 0 to 14 nM wortmannin with varying ATP concentrations from 2.5 to 20 μM. For studies of the time course of PtdIns-3-kinase inhibition, wortmannin 0 to 14 nM, enzyme, and PtdIns were incubated for various times at room temperature before adding [γ-32P]ATP to start the reaction.
Reaction Conditions	0-14 nM wortmannin
Applications	Kinetic analysis demonstrates that wortmannin is a noncompetitive, irreversible inhibitor of phosphatidylinositol-3-kinase, with inactivation being both time- and concentration-dependent.
Cell experiment [2]:
Cell lines	Jurkat cells
Preparation Method	Jurkat-soluble fractions were treated with AX7503 (50 nM) for 60 min with or without preincubation with various concentrations of wortmannin (0.25-50 nM) or LY294002 (10-50,000 nM) for 10 min.
Reaction Conditions	Wortmannin (0.25-50 nM) for 10 min
Applications	PLK1 activity was inhibited by wortmannin with an IC₅₀ value of 24 nM.
Animal experiment [3]:
Animal models	Scid mice
Preparation Method	Oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period.
Dosage form	1 mg/kg for 14 days; 1.5 mg/kg for 5 days + 1.0 mg/kg for 9 days.
Applications	Wortmannin treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation.
References: [1]. Powis G, Bonjouklian R, et al. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Res. 1994 May 1;54(9):2419-23. PMID: 8162590. [2]. Liu Y, Shreder KR, et al. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase. Chem Biol. 2005 Jan;12(1):99-107. doi: 10.1016/j.chembiol.2004.11.009. PMID: 15664519. [3]. Lemke LE, Paine-Murrieta GD, et al. Wortmannin inhibits the growth of mammary tumors despite the existence of a novel wortmannin-insensitive phosphatidylinositol-3-kinase. Cancer Chemother Pharmacol. 1999;44(6):491-7. doi: 10.1007/s002800051123. PMID: 10550570.

Wortmannin is a highly potent direct inhibitor of PI3-kinase specificity originally derived from fungi (1,2). This inhibition is irreversible and non-competitive with an IC50 of 3 nM^[2]^[3]. Wortmannin does not inhibit PI4 kinase, protein kinase C, or protein tyrosine kinases^[4].

In Jurkat cell, at the concentrations of wortmannin commonly used to inhibit PI 3-kinases, PLK1 is also significantly inhibited^[5]. In Swiss 3T3 cells, Wortmannin is a selective and reversible phosphatidylinositol 3-kinase inhibitor with an IC50 value of 1.9 nM^[4].PI3-kinase is involved in the signal transduction pathway responsible for histamine secretion following stimulation of Fc epsilon RI and that wortmannin blocks these responses through direct interaction with the catalytic subunit of this enzyme^[1].

Wortmannin treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation^[6]. Wortmannin inhibits myosin light chain phosphorylation and contraction in rat aorta. As an inhibitor of MLCK, wortmannin can be used as a vasodilator and anti-inflammatory agent^[7].

References:
[1]: Yano H, Nakanishi S, et,al. Inhibition of histamine secretion by wortmannin through the blockade of phosphatidylinositol 3-kinase in RBL-2H3 cells. J Biol Chem. 1993 Dec 5;268(34):25846-56. PMID: 7503989.
[2]: Moon EK, Kim SH, et,al. Autophagy inhibitors as a potential antiamoebic treatment for Acanthamoeba keratitis. Antimicrob Agents Chemother. 2015 Jul;59(7):4020-5. doi: 10.1128/AAC.05165-14. Epub 2015 Apr 20. PMID: 25896709; PMCID: PMC4468686.
[3]: Liu Y, Jiang N, et,al. Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects. J Biol Chem. 2007 Jan 26;282(4):2505-11. doi: 10.1074/jbc.M609603200. Epub 2006 Nov 29. PMID: 17135248.
[4]: Powis G, Bonjouklian R, et,al. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Res. 1994 May 1;54(9):2419-23. PMID: 8162590.
[5]: Liu Y, Shreder KR, et,al. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase. Chem Biol. 2005 Jan;12(1):99-107. doi: 10.1016/j.chembiol.2004.11.009. PMID: 15664519.
[6]: Lemke LE, Paine-Murrieta GD, et,al. Wortmannin inhibits the growth of mammary tumors despite the existence of a novel wortmannin-insensitive phosphatidylinositol-3-kinase. Cancer Chemother Pharmacol. 1999;44(6):491-7. doi: 10.1007/s002800051123. PMID: 10550570.
[7]: Nakanishi S, Kakita S, et,al.Wortmannin, a microbial product inhibitor of myosin light chain kinase. J Biol Chem. 1992 Feb 5;267(4):2157-63. PMID: 1733924.

Cas No.	19545-26-7	SDF
المرادفات	KY 12420
Chemical Name	(1S,6bR,9aS,11R,11bR)-1-(methoxymethyl)-9a,11b-dimethyl-3,6,9-trioxo-3,6,6b,7,8,9,9a,10,11,11b-decahydro-1H-furo[4,3,2-de]indeno[4,5-h]isochromen-11-yl acetate
Canonical SMILES	O=C1[C@](C([H])([H])[C@@]2([H])OC(C([H])([H])[H])=O)(C([H])([H])[H])[C@](C([H])([H])C1([H])[H])([H])C(C3=O)=C2[C@]4(C([H])([H])[H])C5=C3OC([H])=C5C(O[C@]4([H])C([H])([H])OC([H])([H])[H])=O
Formula	C₂₃H₂₄O₈	M.Wt	428.43
الذوبان	≥ 21.42mg/mL in DMSO	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	2.3341 mL	11.6705 mL	23.341 mL
	5 mM	0.4668 mL	2.3341 mL	4.6682 mL
	10 mM	0.2334 mL	1.1671 mL	2.3341 mL

حاسبة المولارية
حاسبة التخفيف
Molecular Weight Calculator

احسب

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal:μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

مراجعات

Review for Wortmannin

Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

5 Star

100%

4 Star

3 Star

2 Star

1 Star

Review for Wortmannin

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

Overall Rating

★

Review Title

المراجعة

اللقب

البريد الإلكتروني

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.

Wortmannin (Synonyms: KY 12420)

مراجعات العميل

GlpBio Citations

Bioactive Compounds Premium Provider

Product has been cited by 2 publications

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

حاسبة المولارية

حاسبة التخفيف

Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Related Video

مراجعات

Wortmannin (Synonyms: KY 12420)

مراجعات العميل

GlpBio Citations

Bioactive Compounds Premium Provider

Product has been cited by 2 publications

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

حاسبة المولارية

حاسبة التخفيف

Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Related Video

Related Products

مراجعات