Cat. No.: HY-164393

ON044580

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ON044580 is a non–ATP-competitive JAK2 and BCR-ABL kinases inhibitor. ON044580 inhibits wild-type (WT) and V617F mutant JAK2 with IC₅₀ values of 1.23 μM, 1.09 μM, respectively. ON044580 also inhibits both WT and T315I mutant BCR-ABL kinases., ON044580 blocks the IL-3–mediated phosphorylation of JAK2 and STAT5, induces apoptosis in Imatinib (HY-15463)-resistant chronic myeloid leukemia (CML). ON044580 can be used for the study of CML, myelodysplasia (MDS) and other myeloproliferative neoplasms.

For research use only. We do not sell to patients.

Purity: 99.11%
CAS No.: 1035199-04-2
Formula: C₂₃H₁₅BrFNO₅S
Molecular Weight:516.34

Storage:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ON044580 Chemical Structure

CAS No.: 1035199-04-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK2-WT

1.23 μM (IC₅₀)

JAK2-V617F

1.09 μM (IC₅₀)

WT BCR-ABL

T315I-BCR-ABL

All JAK Isoforms :

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
K562	GI₅₀	< 1 μM Compound: 6c	Growth inhibition of human K562 cells expressing p210Bcr/Abl after 96 hrs by trypan blue exclusion assay. Growth inhibition of human K562 cells expressing p210Bcr/Abl after 96 hrs by trypan blue exclusion assay.	20188579
DU-145	GI₅₀	1 μM Compound: 6c	Growth inhibition of human DU145 cells after 96 hrs by trypan blue exclusion assay. Growth inhibition of human DU145 cells after 96 hrs by trypan blue exclusion assay.	20188579
K562	IC₅₀	0.5 μM Compound: 6c	Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis. Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis.	20188579
HEL	GI₅₀	0.9 μM	Inhibits the proliferation of HEL cells. Inhibits the proliferation of HEL cells.	20717479
SET-2	GI₅₀	3.0 μM	Inhibits the proliferation of SET-2 cells. Inhibits the proliferation of SET-2 cells.	20717479
K562	IC₅₀	7.94 μM	Inhibition of BCR-ABL kinase activity. Inhibition of BCR-ABL kinase activity.	20717479

In Vitro

ON044580 (0.25-10 μM; 30 min) inhibits recombinant wild-type JAK2 and JAK2-V617F kinase activities with IC₅₀ values of 1.23 μM and 1.09 μM, respectively^[1].
ON044580 (0-10 μM; 30 min) inhibits full-length JAK2 immunoprecipitated from Ba/F3:JAK2V617F cells with an IC₅₀ of approximately 4 μM^[1].
ON044580 (0-20 μM; 30 min) inhibits wild-type BCR-ABL and T315I mutant BCR-ABL kinase activities immunoprecipitated from K562 and 32D:p210T315I cells, with IC₅₀ values of 7.94 μM and 2.08 μM, respectively^[1].
ON044580 (0-20 μM; 2 h) inhibits JAK2 autophosphorylation and STAT5 phosphorylation in IL-3-stimulated Ba/F3:JAK2V617F cells in a concentration-dependent manner^[1].
ON044580 (10 μM; 15-60 min) inhibits IL-3-mediated JAK2 phosphorylation within 15-30 minutes in Ba/F3:JAK2V617F cells^[1].
ON044580 (0-10 μM; 2 h) inhibits STAT3 phosphorylation in U266 multiple myeloma cells (constitutive IL-6 receptor/JAK2/STAT3 pathway) in a dose-dependent manner^[1].
ON044580 (0.5-10 μM; 72 h) inhibits the proliferation of JAK2V617F-expressing cells (Ba/F3:JAK2V617F, HEL, SET-2) with GI₅₀ values of 0.25 μM, 0.9 μM, and 3.0 μM, respectively^[1].
ON044580 (0.5 μM; 2-24 h) induces PARP cleavage in Ba/F3:JAK2V617F cells at 24 h^[1].
ON044580 (0.1-0.5 μM; ex vivo, 48 h) selectively reduces aneuploid (monosomy 7) cells while maintaining/increasing diploid cells in bone marrow mononuclear cells^[1].
ON044580 (1-10 μM; 2 h short-term exposure followed by 96 h recovery) inhibits growth of Ba/F3:JAK2V617F, HEL, and K562 cells in a concentration-dependent manner, while normal mouse bone marrow cells remain unaffected^[1].
ON044580 (0.5-10 μM; ex vivo, 48 h) induces apoptosis in primary CML cells from blast crisis patients refractory to Imatinib (HY-15463)^[1]^[2].
ON044580 (0.25-10 μM; 30 min) inhibits recombinant Abl kinase activity by 50% at 5 μM and 75% at 10 μM^[2].
ON044580 (0.1-10 μM; 16 h) reduces BCR-ABL protein levels and pTyr-JAK2 in Imatinib-sensitive and Imatinib-resistant (T315I, E255K) BCR-ABL+ cells in a dose-dependent manner^[2].
ON044580 (10 μM; 6-16 h) reduces levels of BCR-ABL downstream signaling molecules including STAT3, pTyr705-STAT3, pSer727-STAT3, and Akt in BCR-ABL+ 32D cells^[2].
ON044580 (0-10 μM; 16 h) reduces HSP90α transcript levels in BCR-ABL+ 32D cells^[2].
ON044580 (0.25-10 μM; 16 h) reduces HSP90 protein levels in Imatinib-sensitive and Imatinib-resistant (T315I, E255K) BCR-ABL+ cells^[2].
ON044580 (10 μM; 3 h) disrupts the BCR-ABL/JAK2/HSP90 high molecular weight network complex in BCR-ABL+ 32D cells^[2]. ON044580 (0-10 μM; 48 h) induces apoptosis in Imatinib-sensitive and Imatinib-resistant (T315I, K562-R) BCR-ABL+ cells at concentrations of 1-5 μM^[2].
ON044580 (0.1-0.5 μM; 2 weeks) inhibits colony formation of Imatinib-sensitive and Imatinib-resistant (T315I, E255K) BCR-ABL+ cells in soft agar^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

Ba/F3:JAK2V617F cells (+IL-3)
Concentration:

0.1, 0.5, 1, 5, 10 μM
Incubation Time:

2 h
Result:

Inhibited JAK2 autophosphorylation and STAT5 phosphorylation in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:

Ba/F3:JAK2V617F cells (+IL-3)
Concentration:

10 μM
Incubation Time:

15-60 min
Result:

Inhibited IL-3-mediated JAK2 phosphorylation within 15-30 minutes.

Cell Viability Assay^[1]

Cell Line:

Ba/F3:JAK2V617F, HEL, SET-2 cells
Concentration:

0.5, 1, 2.5, 5, 10 μM
Incubation Time:

72 h
Result:

Inhibited the proliferation of JAK2V617F-expressing cells (Ba/F3:JAK2V617F, HEL, SET-2) with GI50 values of 0.25 μM, 0.9 μM, and 3.0 μM, respectively.

Western Blot Analysis^[1]

Cell Line:

Ba/F3:JAK2V617F
Concentration:

0.5 μM
Incubation Time:

2-24 h
Result:

Induced PARP cleavage.

Western Blot Analysis^[2]

Cell Line:

BCR-ABL+ 32D cells
Concentration:

10 μM
Incubation Time:

6-16 h
Result:

Reduces levels of BCR-ABL downstream signaling molecules including STAT3, pTyr705-STAT3, pSer727-STAT3, and Akt.

Western Blot Analysis^[1]

Cell Line:

BCR-ABL+ 32D cells
Concentration:

1, 5, 10 μM
Incubation Time:

16 h
Result:

Reduced HSP90 protein levels.

RT-PCR^[2]

Cell Line:

BCR-ABL+ 32D cells
Concentration:

1, 5, 10 μM
Incubation Time:

16 h
Result:

Reduced HSP90α transcript levels.

Apoptosis Analysis^[2]

Cell Line:

BCR-ABL+ cells (WT, T315I, K562-R)
Concentration:

2.5, 5, 10 μM
Incubation Time:

48 h
Result:

Induced apoptosis in Imatinib-sensitive and Imatinib-resistant (T315I, K562-R) BCR-ABL+ cells.

Cell Proliferation Assay^[2]

Cell Line:

BCR-ABL+ cells (WT, T315I, E255K)
Concentration:

0.01, 0.05, 0.1, 0.5, 1 μM
Incubation Time:

2 weeks
Result:

Inhibited colony formation.

Chemical Information

CAS No. 1035199-04-2
Appearance Solid
Molecular Weight 516.34
Formula C₂₃H₁₅BrFNO₅S
Color Off-white to light yellow
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jatiani SS, 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. [Content Brief]

[2]. Samanta AK, et al. Destabilization of Bcr-Abl/Jak2 Network by a Jak2/Abl Kinase Inhibitor ON044580 Overcomes Drug Resistance in Blast Crisis Chronic Myelogenous Leukemia (CML). Genes Cancer. 2010 Apr;1(4):346-59. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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ON044580

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

All JAK Isoforms

All Bcr-Abl Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

ON044580 Related Classifications

HY-164393 Related Classifications