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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 -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].

Product Specifications

CAS Number

1035199-04-2

UNSPSC

12352005

Target

Apoptosis; Bcr-Abl; JAK

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/on044580.html

Purity

99.11

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

Molecular Formula

C23H15BrFNO5S

Molecular Weight

516.34

References & Citations

[1]Shashidhar S Jatiani, et al. A Non-ATP-Competitive Dual Inhibitor of JAK2 and BCR-ABL Kinases: Elucidation of a Novel Therapeutic Spectrum Based on Substrate Competitive Inhibition. Genes Cancer. 2010 Apr;1 (4) :331-45.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

Bcr-Abl; JAK2

Available Sizes

Frequently Asked Questions

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