PIT-1

SKU: orb1704223

Description

PIT-1 is a selective PIP3 antagonist that suppresses the PI3K/Akt pathway by blocking PIP3 binding to Akt's PH domain. This inhibition induces apoptosis and reduces cancer cell viability, making it a valuable tool for studying oncogenic signalling in both cellular and animal models of cancer.

Research Area

Cell Biology

Key Properties

• CAS Number: 53501-41-0
• MW: 351.76
• Purity: >98%
• Formula: C₁₄H₁₀ClN₃O₄S
• SMILES: OC1=C(Cl)C=C(C=C1NC(=S)NC(=O)C1=CC=CC=C1)[N+]([O-])=O
• Target: Kinase
• Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 3 mg/ml).

Bioactivity

• In Vivo:
  In a breast cancer xenograft model using nude mice, PIT-1 (intraperitoneal injection) significantly inhibited tumor growth, reducing tumor volume by approximately 60% compared to the control group, with no apparent toxicity.
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• In Vitro:
  In breast cancer cell lines such as MCF-7, PIT-1 (10–100 μM, 24–48 h) induces apoptosis, reduces cell viability, and significantly downregulates the expression of Pit-1 target genes, including GH, PRL, and GHRHR. Additionally, PIT-1 upregulates pro-apoptotic genes such as Bax and activates caspase-3, suggesting PIT-1 induces apoptosis through a mitochondrial pathway.
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Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PIT 1, PIT1, PIT-1

Compound Identifiers

PubChem CID

3664359