2. JAK/STAT Signaling Stem Cell/Wnt Metabolic Enzyme/Protease Apoptosis
  3. STAT MMP Apoptosis
  4. STAT3-IN-52

STAT3-IN-52 (Compound 9) is a selective and orally active signal transducer and activator of transcription 3 (STAT3) inhibitor. STAT3-IN-52 binds to the pY705 site of STAT3 (Ki = 440 nM), blocking the phosphorylation and dimerization of STAT3. STAT3-IN-52 shows strong cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 = 0.7 μM), medulloblastoma UW426, pancreatic cancer BKPC3 cells. STAT3-IN-52 can induce cell apoptosis, inhibit the STAT3 nuclear transport and DNA binding activity and downregulate the expression of the STAT3 target gene MMP9. STAT3-IN-52 can be used for research related to STAT3 abnormal activation in cancer.

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STAT3-IN-52

STAT3-IN-52 Chemical Structure

CAS No. : 1556861-34-7

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STAT3-IN-52 Related Antibodies

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Description

STAT3-IN-52 (Compound 9) is a selective and orally active signal transducer and activator of transcription 3 (STAT3) inhibitor. STAT3-IN-52 binds to the pY705 site of STAT3 (Ki = 440 nM), blocking the phosphorylation and dimerization of STAT3. STAT3-IN-52 shows strong cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 = 0.7 μM), medulloblastoma UW426, pancreatic cancer BKPC3 cells. STAT3-IN-52 can induce cell apoptosis, inhibit the STAT3 nuclear transport and DNA binding activity and downregulate the expression of the STAT3 target gene MMP9. STAT3-IN-52 can be used for research related to STAT3 abnormal activation in cancer[1].

IC50 & Target[1]

STAT3

440 nM (Ki)

MMP-9

 

Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ Vz CL MRT0-t MRT0-∞ F
Rat[1] 1 mg/kg i.v. 0.71 h 0.033 h 359.0 ng/mL 189.0 ng·h/mL 199.2 ng·h/mL 4944.2 mL/kg 5261.7 mL/h/kg 0.55 h 0.71 h /
Rat[1] 10 mg/kg p.o. 1.98 h 0.5 h 540.3 ng/mL 850.0 ng·h/mL 889.0 ng·h/mL 32092.5 mL/kg 11766.8 mL/h/kg 1.87 h 2.25 h 44.7 %
Molecular Weight

412.46

Formula

C20H20N4O4S
CAS No.
SMILES

O=S(C(C=CC=C1C(C(NC2=CC=CC=C2N3CCNCC3)=C4)=O)=C1C4=O)(N)=O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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STAT3-IN-52 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STAT3-IN-521556861-34-7STATMMPApoptosisMatrix metalloproteinasesInhibitorinhibitorinhibit

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