Home JAK/STAT STAT inhibitor BP-1-102 For research use only.

BP-1-102

BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor, binds Stat3 with an affinity Kd of 504 nM and blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM.

BP-1-102 Chemical Structure

BP-1-102 Chemical Structure

CAS No. 1334493-07-0

Purity & Quality Control

BP-1-102 Related Products

Signaling Pathway

STAT Signaling Pathways

STAT Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
30M cells Cytotoxicity assay 3 days Cytotoxicity against human 30M cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=2 μM 24900612
OCI-AML2 cells Cytotoxicity assay 72 h Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay, IC50=10 μM 23968501
MDA468 cells Cytotoxicity assay Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay, EC50=10.9 μM 21788134
JJN-3 cells Cytotoxicity assay 72 h Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay, EC50=16.7 μM 21788134
DU145 cells Cytotoxicity assay 72 h Cytotoxicity against human DU145 cells after 72 hrs by MTS assay, EC50=22.7 μM 21788134
147EF cells Function assay 0.1-1 μM 3 h Inhibition of AKT phosphorylation in human 147EF cells at 0.1 to 1 uM after 3 hrs by Western blotting analysis 24900612
Click to View More Cell Line Experimental Data

Biological Activity

Description BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor, binds Stat3 with an affinity Kd of 504 nM and blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM.
Targets
STAT3 [1]
504 nM(Kd)
In vitro
In vitro

BP-1-102 binds Stat3 with an affinity (KD) of 504 nM, blocks Stat3-phospho-tyrosine (pTyr) 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, which is identified as a Stat3 target gene that promotes Stat3-mediated breast tumor cell migration and invasion. Treatment of breast cancer cells with BP-1-102 further blocks Stat3–NF-κB cross-talk, the release of granulocyte colony-stimulating factor, soluble intercellular adhesion molecule 1, macrophage migration-inhibitory factor/glycosylation-inhibiting factor, interleukin 1 receptor antagonist, and serine protease inhibitor protein 1, and the phosphorylation of focal adhesion kinase and paxillin, while enhancing E-cadherin expression. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM and preferentially inhibits Stat3-Stat3, over Stat1-Stat3, Stat1-Stat1, or Stat5-Stat5 DNA-binding activity. BP-1-102 has little or no effect on phospho-Shc, Src, Jak-1/2, Erk1/2, or Akt levels[1].
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 c-Myc / Cyclin D1 / Survivin 30720080
In Vivo
In vivo

Intravenous or oral gavage delivery of BP-1-102 furnishes micromolar or microgram levels in tumor tissues and inhibits growth of human breast and lung tumor xenografts and modulates Stat3 activity, Stat3 target genes, and soluble factors in vivo. BP-1-102 selectively suppresses growth, survival, malignant transformation, migration, and invasion of malignant cells harboring constitutively active stat3. BP-1-102 is detectable at micromolar concentrations in plasma and in micrograms in tumor tissues[1].
Animal Research Animal Models Athymic nude mice
Dosages 1 or 3 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 626.59 Formula

C29H27F5N2O6S
CAS No. 1334493-07-0 SDF Download BP-1-102 SDF
Smiles CN(CC(=O)N(CC1=CC=C(C=C1)C2CCCCC2)C3=CC(=C(C=C3)C(=O)O)O)S(=O)(=O)C4=C(C(=C(C(=C4F)F)F)F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (159.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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