GLPBio

Wortmannin

Catalog No.: GC12338Purity:>98.00%Synonyms: KY 12420
COASDSData Sheet
Wortmannin is a potent, selective, and irreversible PI3K inhibitor with an IC50 value of 4.2nM.

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

Wortmannin
Cas No.: 19545-26-7
10mM (in 1mL DMSO)In Stock
$82.00
1
5mgIn Stock
$62.00
1
10mgIn Stock
$90.00
1
20mgIn Stock
$145.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

3 publicationsPublications from researchers using this product

Description

Wortmannin is a potent, selective, and irreversible PI3K inhibitor with an IC50 value of 4.2nM[1]. Wortmannin is an effective radiosensitizer that irreversibly inhibits DNA-dependent protein kinase (DNA-PK) and ataxia telangiectasia mutated (ATM) with IC50 values of 16nM and 150nM, respectively[2]. By inhibiting the activity of PI3K, Wortmannin regulates the expression of survivin, cyclinD1, PI3K and p-Akt, and reduces cell migration activity and induces the expression of E-cadherin[3]. Wortmannin has been widely used to inhibit the secretion of histamine in cells[4].

In vitro, Wortmannin treatment for 24 hours significantly inhibited the growth of K562 cells, with an IC50 value of 25nM[5]. Treatment with 2µM Wortmannin for 24 hours significantly induced apoptosis in MCF-7 cells, accompanied by chromatin condensation, nuclear fragmentation, reactive oxygen species, and membrane blebbing[6]. Treatment of MDA-MB-231 cells with 200nM Wortmannin for 4 hours significantly inhibited the upregulation of Akt phosphorylation, NF-κB, MMP-9, and IL-8[7].

In vivo, Wortmannin treatment via oral administration at a dose of 1.5mg/kg/day for 22 days reduced insulin signaling and mortality in seizure-prone Pcmt1−/− mice[8]. Daily intraperitoneal injection of Wortmannin at a dose of 1mg/kg/day for 28 days significantly inhibited tumor growth in the Colo-699 xenograft mouse model and prolonged the survival time of the mice[9].

References:
[1] Walker E H, Pacold M E, Perisic O, et al. Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine[J]. Molecular cell, 2000, 6(4): 909-919.
[2] Sarkaria J N, Tibbetts R S, Busby E C, et al. Inhibition of phosphoinositide 3-kinase related kinases by the radiosensitizing agent wortmannin[J]. Cancer research, 1998, 58(19): 4375-4382.
[3] Bani N, Rahmani F, Shakour N, et al. Wortmannin inhibits cell growth and induces apoptosis in colorectal cancer cells by suppressing the PI3K/AKT pathway[J]. Anti-Cancer Agents in Medicinal Chemistry-Anti-Cancer Agents), 2024, 24(12): 916-927.
[4] Yano H, Nakanishi S, Kimura K, et al. Inhibition of histamine secretion by wortmannin through the blockade of phosphatidylinositol 3-kinase in RBL-2H3 cells[J]. Journal of Biological Chemistry, 1993, 268(34): 25846-25856.
[5] Wu Q, Chen Y, Cui G, et al. Wortmannin inhibits K562 lukemic cells by regulating PI3k/Akt channel in vitro[J]. Journal of Huazhong University of Science and Technology [Medical Sciences], 2009, 29(4): 451-456.
[6] Akter R, Hossain M Z, Kleve M G, et al. Wortmannin induces MCF-7 breast cancer cell death via the apoptotic pathway, involving chromatin condensation, generation of reactive oxygen species, and membrane blebbing[J]. Breast Cancer: Targets and Therapy, 2012: 103-113.
[7] Li J, Li F, Wang H, et al. Wortmannin reduces metastasis and angiogenesis of human breast cancer cells via nuclear factor-κB-dependent matrix metalloproteinase-9 and interleukin-8 pathways[J]. Journal of International Medical Research, 2012, 40(3): 867-876.
[8] MacKay K B, Lowenson J D, Clarke S G. Wortmannin reduces insulin signaling and death in seizure-prone Pcmt1−/− mice[J]. 2012.
[9] Boehle A, Kurdow R, Boenicke L, et al. Wortmannin inhibits growth of human non-small-cell lung cancer in vitro and in vivo[J]. Langenbeck's archives of surgery, 2002, 387(5): 234-239.

Protocol

Cell experiment [1]:

Cell lines

K562 cells

Preparation Method

K562 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum, 100U/ml penicillin, and 100μg/ml streptomycin at 37°C with 5% CO2 and 95% saturated atmospheric humidity. Cells were seeded into 96-well microplates at a density of 5×105 cells/ml for 24h. Various concentrations of Wortmannin (0, 6.25, 12.5, 25, 50, and 100nM) were added to each well. After 24h of incubation, cell viability was analyzed.

Reaction Conditions

0, 6.25, 12.5, 25, 50, and 100nM; 24h

Applications

Wortmannin treatment significantly reduced the cell viability of K562 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Female SCID-bg mice

Preparation Method

Female SCID-bg mice (6 weeks old; 18-20g) were housed under standard laboratory conditions on a 12-hour light/dark cycle (lights on at 7:00 am), constant temperature (23±2°C), and constant humidity (60±5%), ad libitum food and water. For induction of intrapulmonary tumor growth, mice were anesthetized by intraperitoneal injection of 240mg/kg Avertin, and 2×106 Colo-699 cells were introduced below the visceral pleura. Daily intraperitoneal injection of Wortmannin at a dose of 1mg/kg for 28 days was performed, after which the tumor volume was analyzed in mice.

Dosage form

1mg/kg/day; 28 days; i.p.

Applications

Wortmannin treatment inhibited tumor growth in the Colo-699 xenograft mouse models.

References:
[1] Wu Q, Chen Y, Cui G, et al. Wortmannin inhibits K562 lukemic cells by regulating PI3k/Akt channel in vitro[J]. Journal of Huazhong University of Science and Technology [Medical Sciences], 2009, 29(4): 451-456.
[2] Boehle A, Kurdow R, Boenicke L, et al. Wortmannin inhibits growth of human non-small-cell lung cancer in vitro and in vivo[J]. Langenbeck's archives of surgery, 2002, 387(5): 234-239.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Biological Data

1 / 2

Chemical Properties

CAS No.
19545-26-7
Synonyms
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
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
Molecular Formula
C23H24O8
Molecular Weight
428.43
Solubility
≥ 21.42mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

Reviews

Review for Wortmannin

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%