BP-1-102

SKU: orb1226523

Description

An orally bioavailable, small-molecule inhibitor of STAT3 with Kd of 504 nM; blocks Stat3-pTyr peptide interactions and Stat3 activation at 4-6.8 uM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells; suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and KLF8, blocks Stat3-NF-κB cross-talk, and enhances E-cadherin expression; inhibits growth of human breast and lung tumor xenografts.

Key Properties

• CAS Number: 1334493-07-0
• MW: 626.5915
• Purity: >98% (HPLC)
• Formula: C₂₉H₂₇F₅N₂O₆S
• SMILES: O=C(O)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1O
• Target: STAT
• Solubility: DMSO: ≥ 33 mg/mL

Bioactivity

• In Vivo:
  Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth.
• In Vitro:
  BP-1-102 binds Stat3 with an affinity KD of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8.

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

BP-1-102 | BP1-102 | BP 1-102 | BP1102

Quick Database Links

Gene Symbol

STAT