2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. JAK Bcr-Abl Apoptosis
  4. ON044580

ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling.

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ON044580 Chemical Structure

ON044580 Chemical Structure

CAS No. : 1035199-04-2

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Description

ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling[1].

IC50 & Target[1]

JAK2-WT

1.23 μM (IC50)

JAK2-V617F

1.09 μM (IC50)

WT BCR-ABL

 

T315I-BCR-ABL

 

Molecular Weight

516.34

Formula

C23H15BrFNO5S
CAS No.
SMILES

O=C(C1=CC=C(C(O)=O)C=C1)/C(SCC2=CC=C(Br)C=C2)=C\C3=CC=C(F)C([N+]([O-])=O)=C3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ON044580 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:

ON0445801035199-04-2ON 044580ON-044580JAKBcr-AblApoptosisJanus kinaseV617Fantiproliferativeleukemic cellschronic myelogenous leukemiaCMLT315ImyeloproliferativeInhibitorinhibitorinhibit

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