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Wortmannin

Catalog No. T6283 CAS 19545-26-7

Synonyms: SL-2052, KY-12420

Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8/48 nM) that blocks autophagy.

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Wortmannin, CAS 19545-26-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 198.00
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.76%

Purity: 98.86%

Purity: 97.02%

Purity: 95.84%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8/48 nM) that blocks autophagy.
Targets&IC50	PI3K:3 nM, DNA-PK:16 nM, ATM:150 nM
In vitro	METHODS: Human breast cancer cells MCF-7 were treated with Wortmannin (50-500 nM) for 24 h. Cell death was detected by Trypan blue exclusion assay. RESULTS: Wortmannin induced cell death in MCF-7 cells in a concentration-dependent manner with an IC50 of 400 nM. [1] METHODS: Human breast cancer cells MCF-7 were treated with Wortmannin (6.25-50 nM) for 24 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Concentration-dependent reduction of p-Akt and NF-κB p65 expression was induced by Wortmannin. [2]
In vivo	METHODS: To determine whether activation of the insulin pathway and brain enlargement were responsible for fatal seizures, Wortmannin (1.5 mg/kg) was administered orally to Pcmt1-/- mice once a day for twenty-two days. RESULTS: Wortmannin reduced the average brain size of Pcmt1-/- mice to within 6% of that of controls and nearly doubled the lifespan of Pcmt1-/- mice, with a survival rate of 60% of the original population. [3] METHODS: To investigate antitumor activity, Wortmannin (0.25-1 mg/kg) was injected intravenously three times a week for three weeks into SCID mice bearing the human breast cancer tumor MDA-MB-231. RESULTS: Wortmannin significantly inhibited tumor metastasis and angiogenesis. [4]

Synonyms	SL-2052, KY-12420
Molecular Weight	428.43
Formula	C23H24O8
CAS No.	19545-26-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 2.1 mg/mL (5 mM)), Heating is recommended.

DMSO: 21.4 mg/mL (50 mM)

References and Literature

1. Akter R, 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. Breast Cancer (Dove Med Press). 2012 Jul 13;4:103-13. 2. Yun J, et al. Wortmannin inhibits proliferation and induces apoptosis of MCF-7 breast cancer cells. Eur J Gynaecol Oncol. 2012;33(4):367-9. 3. MacKay KB, et al. Wortmannin reduces insulin signaling and death in seizure-prone Pcmt1-/- mice. PLoS One. 2012;7(10):e46719. 4. Li J, 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 Int Med Res. 2012;40(3):867-76. 5. Zhang H, Cui Z, Cheng D, et al. RNF186 regulates EFNB1 (ephrin B1)-EPHB2-induced autophagy in the colonic epithelial cells for the maintenance of intestinal homeostasis[J]. Autophagy . 2020

Citations

1. Zhang H, Cui Z, Cheng D, et al. RNF186 regulates EFNB1 (ephrin B1)-EPHB2-induced autophagy in the colonic epithelial cells for the maintenance of intestinal homeostasis. Autophagy. 2021 Oct;17(10):3030-3047 2. Ly T T G, Yun J, Ha J S, et al. Inhibitory Effect of Etravirine, a Non-Nucleoside Reverse Transcriptase Inhibitor, via Anterior Gradient Protein 2 Homolog Degradation against Ovarian Cancer Metastasis. International Journal of Molecular Sciences. 2022, 23(2): 944. 3. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Scientific Reports. 2018 Oct 8;8(1):14969 4. Gao Y, Xiong J, Chu Q Z, et al. PDZD8-mediated lipid transfer at contacts between the ER and late endosomes/lysosomes is required for neurite outgrowth. Journal of Cell Science. 2022 Mar 1;135(5):jcs255026. doi: 10.1242/jcs.255026. Epub 2021 Apr 20. 5. Wang C, Wang T, Hu R, et al.9-Butyl-Harmol Exerts Antiviral Activity against Newcastle Disease Virus through Targeting GSK-3β and HSP90β.Journal of Virology.2023: e01984-22. 6. Wang T, Wang L, Li W, et al.Fowl adenovirus serotype 4 enters leghorn male hepatocellular cells via the clathrin-mediated endocytosis pathway.Veterinary Research.2023, 54(1): 1-14. 7. Wang H, Ye J, Peng Y, et al.CKLF induces microglial activation via triggering defective mitophagy and mitochondrial dysfunction.Autophagy.2023 (just-accepted). 8. Xiong Q, Sun H, Wang Y, et al.Lipid droplet accumulation in Wdr45-deficient cells caused by impairment of chaperone-mediated autophagic degradation of Fasn.Lipids in Health and Disease.2024, 23(1): 91.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Kinase Inhibitor Library Preclinical Compound Library Glycolysis Compound Library Anti-Obesity Compound Library Anti-Prostate Cancer Compound Library NO PAINS Compound Library Anti-Pancreatic Cancer Compound Library Anti-Infection Compound Library

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Keywords

Wortmannin 19545-26-7 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism Microbiology/Virology PI3K/Akt/mTOR signaling Antibiotic PI3K Serine/threonin kinase PLK DNA-PK ATM/ATR KY12420 SL 2052 SL-2052 inhibit Polo-like Kinase (PLK) KY 12420 Phosphoinositide 3-kinase Inhibitor SL2052 KY-12420 inhibitor

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