1. JAK/STAT Signaling
    Stem Cell/Wnt
  2. STAT
  3. BP-1-102

BP-1-102 

Cat. No.: HY-100493 Purity: 99.36%
Handling Instructions

BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.

For research use only. We do not sell to patients.

BP-1-102 Chemical Structure

BP-1-102 Chemical Structure

CAS No. : 1334493-07-0

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 131 In-stock
Estimated Time of Arrival: December 31
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BP-1-102 purchased from MCE. Usage Cited in: Cell Commun Signal. 2020 Jul 8;18(1):104.

    Immunoblotting analysis of pulmonary STAT3 and pY-STAT3 in mice 24 h after CLP with BP-1-102 (BP) administration. BP downregulates the elevated pY-STAT3 level in the mouse lung 24 h after CLP.

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    Description

    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.

    IC50 & Target[1]

    STAT3

    6.8 μM (IC50)

    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[1].

    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[2]. 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[1].

    Molecular Weight

    626.59

    Formula

    C₂₉H₂₇F₅N₂O₆S

    CAS No.

    1334493-07-0

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (52.67 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5959 mL 7.9797 mL 15.9594 mL
    5 mM 0.3192 mL 1.5959 mL 3.1919 mL
    10 mM 0.1596 mL 0.7980 mL 1.5959 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.99 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.99 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    Proliferating cells in 6- or 96-well plates are treated once with 0-30 μM BP-1-102 for 24 h or with 10 μM BP-1-102 for up to 96 h. Viable cells are counted by trypan blue exclusion/phase-contrast microscopy or assessed by a cell proliferation kit[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice: Athymic nude mice with established tumors are grouped and then given BP-1-102 (in 0.05% DMSO in water) at 1 or 3mg/kg (i.v.) every 2 or every 3 d or 3 mg/kg (oral gavage, 100 μL) every day for 15 or 20 d. Animals are monitored every day, and tumor sizes are measured with calipers and body weights are taken every 2 or 3 d. For each treatment group, the tumor volumes for each set of measurements are statistically analyzed in comparison with the control group using a paired T test[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    BP-1-102STATInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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