Wortmannin

SKU: orb1225783

Description

A potent PI3K inhibitor with IC50 3 nM, does not inhibit PI4K activity; inhibits both Fc epsilon RI-mediated histamine secretion and leukotriene release up to 80% with IC50 of 2.0 and 3.0 nM, respectively; Also inhibits DNA-PK and MLCK.(In Vitro):Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively. Wortmannin prevents nuclear entry of YAP.(In Vivo):Wortmannin (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) 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.

Key Properties

• CAS Number: 19545-26-7
• MW: 428.4319
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₄O₈
• SMILES: CC(O[C@@H](C1=C2C(C3=C4C(C(O[C@H](COC)[C@]14C)=O)=CO3)=O)C[C@]5(C)C(CC[C@]52[H])=O)=O
• Target: PI3K
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Wortmannin (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) 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. Animal model: Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancer xenograft. Dosage: 1 mg/kg and 1.5 mg/kg. Administration: Oral gavage; daily; one group 1 mg/kg for 14 days; second group 1.5 mg/kg for 5 days then 1.0 mg/kg for 9 days. Result: The growth rate of the treated tumors was significantly slower during drug administration than that of nontreated tumors.
  Read more...
• In Vitro:
  Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively. Wortmannin prevents nuclear entry of YAP. Cell Proliferation Assa Cell line: K562 cells. Concentration: 0, 6.25, 12.5, 25, 50 and 100 nM Incubation time: 0, 24, 48 and 72 hours. Result: Inhibited the K562 cells proliferation. The IC50 value at 24 hour, 48 hour, and 72 hour was 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SL-2052 | KY-12420

Quick Database Links

Gene Symbol

PI3K