1334493-07-0

Usage

Uses

Used in Oncology:
BP-1-102 is used as an antitumor agent for its ability to inhibit the STAT3 protein, which is involved in the development of various cancers. By targeting this protein, BP-1-102 can potentially suppress tumor growth and progression, making it a valuable compound in the fight against cancer.
Used in Drug Development for B Cell Non-Hodgkin Lymphoma:
BP-1-102 is used as a therapeutic agent for the treatment of Waldenstrom macroglobulinemia, a rare form of B cell non-Hodgkin lymphoma. Its selective inhibition of STAT3 makes it a promising candidate for the development of targeted therapies for this specific type of cancer.
Used in Research and Development of STAT3 Inhibitors:
BP-1-102 serves as a valuable tool in the research and development of new STAT3 inhibitors. Its potent and selective inhibition of the STAT3 protein can help researchers better understand the role of this protein in cancer development and identify potential therapeutic targets for the treatment of various malignancies.

Upstream product

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• 1455006-13-9 benzyl 4-(2-amino-N-(4-cyclohexylbenzyl)acetamido)-2-(benzyloxy)benzoate 
• 1455006-12-8 benzyl 4-(2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-N-(4-cyclohexylbenzyl)acetamido)-2-(benzyloxy)benzoate 
• 65-49-6 4-Aminosalicylic acid 
• 1334493-20-7 benzyl 2-(benzyloxy)-4-(N-(4-cyclohexylbenzyl)-2-(methylamino)-acetamido)benzoate 
• 1334493-18-3 benzyl 2-(benzyloxy)-4-(N-(4-cyclohexylbenzyl)-2-(2,2,2-trifluoro-N-methylacetamido)acetamido)benzoate 
• 1241833-16-8 benzyl 2-(benzyloxy)-4-((4-cyclohexylbenzyl)amino)benzoate 
• 1241832-99-4 benzyl 4-amino-2-(benzyloxy)benzoate 
• 1334493-48-9 benzyl 2-(benzyloxy)-4-(N-(4-cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)benzoate 

Relevant academic research and scientific papers

Design, synthesis, and in?vitro evaluation of BP-1-102 analogs with modified hydrophobic fragments for STAT3 inhibition

Twelve novel analogs of STAT3 inhibitor BP-1-102 were designed and synthesised with the aim to modify hydrophobic fragments of the molecules that are important for interaction with the STAT3 SH2 domain. The cytotoxic activity of the reference and novel co

Substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs as inhibitors of STAT protein

In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the com

Inhibiting aberrant signal transducer and activator of transcription protein activation with tetrapodal, small molecule Src homology 2 domain binders: Promising agents against multiple myeloma

The signal transducer and activator of transcription (STAT) proteins represent a family of cytoplasmic transcription factors that regulate a pleiotropic range of biological processes. In particular, Stat3 protein has attracted attention as it regulates the expression of genes involved in a variety of malignant processes, including proliferation, survival, migration, and drug resistance. Multiple myeloma (MM) is an incurable hematologic malignancy that often exhibits abnormally high levels of Stat3 activity. Although current treatment strategies can improve the clinical management of MM, it remains uniformly incurable with a dismal median survival time post-treatment of 3-4 years. Thus, novel targeted therapeutics are critically needed to improve MM patient outcomes. We herein report the development of a series of small molecule Stat3 inhibitors with potent anti-MM activity in vitro. These compounds showed high-affinity binding to Stat3's SH2 domain, inhibited intracellular Stat3 phosphorylation, and induced apoptosis in MM cell lines at low micromolar concentrations.

Potent targeting of the STAT3 protein in brain cancer stem cells: A promising route for treating glioblastoma

The STAT3 gene is abnormally active in glioblastoma (GBM) and is a critically important mediator of tumor growth and therapeutic resistance in GBM. Thus, for poorly treated brain cancers such as gliomas, astrocytomas, and glioblastomas, which harbor constitutively activated STAT3, a STAT3-targeting therapeutic will be of significant importance. Herein, we report a most potent, small molecule, nonphosphorylated STAT3 inhibitor, 31 (SH-4-54) that strongly binds to STAT3 protein (KD = 300 nM). Inhibitor 31 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations. Moreover, in vivo, 31 exhibited blood-brain barrier permeability, potently controlled glioma tumor growth, and inhibited pSTAT3 in vivo. This work, for the first time, demonstrates the power of STAT3 inhibitors for the treatment of BTSCs and validates the therapeutic efficacy of a STAT3 inhibitor for GBM clinical application.

Identification of a non-phosphorylated, cell permeable, small molecule ligand for the Stat3 SH2 domain

Signal transducer and activator of transcription 3 (Stat3) protein is a cytosolic transcription factor that is aberrantly activated in numerous human cancers. Inhibitors of activated Stat3-Stat3 protein complexes have been shown to hold therapeutic promis