Wortmannin

SKU: orb1300904

Description

Wortmannin is a potent, covalent PI3K inhibitor (IC50=3 nM) that also inhibits PlK1 and PlK3, thereby blocking autophagy. This small molecule is widely used in biochemical and cell-based research to study signaling pathways, autophagy, and cellular metabolism in both in vitro and in vivo models.

Research Area

Cell Biology

Key Properties

• CAS Number: 19545-26-7
• MW: 428.44
• Purity: >98%
• Formula: C₂₃H₂₄O₈
• SMILES: C[C@@]12C3=C([C@]4([C@](C)(C[C@H]3OC(C)=O)C(=O)CC4)[H])C(=O)C5=C1C(C(=O)O[C@@H]2COC)=CO5
• Target: Kinase
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml).

Bioactivity

• Target IC50:
  DNA-PK:16 nM|MLCK:200 nM|PI3K:3 nM|ATR:1.8 μM|PLK3:48 nM|ATM:150 nM
• 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. 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.
• 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. 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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Antibiotic, ATR, ATM, ATM/ATR, Autophagy, DNA-PK, DNAPK, KY 12420, KY12420, KY-12420, inhibit, Polo-like Kinase (PLK), PLK, MLCK, Inhibitor, SL 2052, SL2052, SL-2052, Serinekinase, threonin kinase, threoninkinase, Serine kinase, Phosphoinositide 3-kinase, Wortmannin, PI3K

Compound Identifiers

PubChem CID

5691