ISA-2011B

SKU: orb1308184

Description

ISA-2011B is a small molecule inhibitor targeting PIP5K1α, a kinase implicated in cancer cell signaling. It is utilized in anticancer research to investigate tumor proliferation and metastasis in both cellular and animal models.

Key Properties

• CAS Number: 1395347-24-6
• MW: 423.85
• Purity: >99.99% (May vary between batches)
• Formula: C₂₂H₁₈ClN₃O₄
• SMILES: [H][C@@]12Cc3cc4OCOc4cc3[C@H](N1C(=O)CN(C)C2=O)c1c[nH]c2ccc(Cl)cc12
• Target: Others
• Solubility: DMSO:100 mg/mL (235.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.44 mM)

Bioactivity

• In Vivo:
  Overexpression of AR-V7 enhances PIP5K1α levels, accelerating prostate cancer (PCa) growth in xenograft mice. Conversely, the PIP5K1α inhibitor ISA-2011B significantly curtails the proliferation and invasiveness of AR-V7 overexpressing xenograft tumors. ISA-2011B effectively impedes tumor cell growth in xenograft mice by targeting the PIP5K1α-related PI3K/AKT pathways, including those responsible for survival, proliferation, and invasion. Furthermore, ISA-2011B interferes with AR-V7 protein stabilization through its dependency on PIP5K1α, thereby hindering the aggressive growth of AR-V7-high tumors in xenograft models.
• In Vitro:
  ISA-2011B significantly decreases AR-V7 and CDK1 levels in both the nucleus and cytoplasm of 22Rv1 cells, demonstrating strong binding affinity towards PIP5K1α and both MARK1 and MARK4 among 460 kinases. In PC-3 cells, ISA-2011B treatment reduces PIP5K1α expression by 78.6% and eliminates nuclear AR expression without affecting cytoplasmic AR. Additionally, ISA-2011B markedly lowers the proliferation rates of PC-3 cells to 58.77%, 48.65%, and 21.62% at doses of 10, 20, and 50 μM, respectively, compared to controls.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, ISA 2011B, ISA2011B, ISA-2011B, Inhibitor, PIP5K1α

Compound Identifiers

PubChem CID

49853637