5.30153
JAK2 Inhibitor X, FLLL32
Synonym(s):
JAK2 Inhibitor X, FLLL32, STAT3 Signaling Inhibitor, FLLL32
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About This Item
Empirical Formula (Hill Notation):
C28H32O6
CAS Number:
Molecular Weight:
464.55
UNSPSC Code:
12352200
NACRES:
NA.77
Assay
≥98% (HPLC)
Quality Level
form
powder
potency
5 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
General description
A cell permeable diketone analog of curcumin that acts as a specific inhibitor of JAK2 (~ 5 µM) and blocks STAT3 phosphorylation in MDA-MB-231 breast and PANC-1 pancreatic cancer cells. However, it does not affect STAT3 phosphorylation in normal human mammary epithelial cells or human pancreatic duct epithelial cells. Does not block the activity of tyrosine kinases containing SH2 and SH2-SH3 domains and several other kinases, such as Akt2, Cdk2-cyclin D1, EGFR kinase, Met, and EbrB2/Her2 kinase (IC50 >100 µM). Also shown to block DNA binding activity of STAT3. Significantly reduces the viability and invasion capacity of various cancer cells (IC50 = 640 nM; 110 nM, 140 nM, 600 nM, 400 nM in PANC-1, HPAC, MDA-MB-231, SK-BR3, and SUM-159 cells, respectively) and induces apoptosis. Shown to significantly reduce tumor burdens in the MDA-MB-231 xenografted mice.
A cell permeable diketone analog of curcumin that acts as a specific inhibitor of JAK2 (~ 5 µM) and blocks STAT3 phosphorylation in MDA-MB-231 breast and PANC-1 pancreatic cancer cells. However, it does not affect STAT3 phosphorylation in normal human mammary epithelial cells or human pancreatic duct epithelial cells. Does not block the activity of tyrosine kinases containing SH2 and SH2-SH3 domains and several other kinases, such as Akt2, Cdk2-cyclin D1, EGFR kinase, Met, and EbrB2/Her2 kinase (IC50 >100 µM). Also shown to block DNA binding activity of STAT3. Significantly reduces the viability and invasion capacity of various cancer cells (IC50 = 640 nM; 110 nM, 140 nM, 600 nM, 400 nM in PANC-1, HPAC, MDA-MB-231, SK-BR3, and SUM-159 cells, respectively) and induces apoptosis. Shown to significantly reduce tumor burdens in the MDA-MB-231 xenografted mice.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
JAK2
JAK2
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Wu, J., et al. 2014. Oncogene33,173.
Onimoe, G., et al. 2012. Invest. New Drugs30, 916.
Li, L., et al. 2010. Cancer Res.70, 2445.
Onimoe, G., et al. 2012. Invest. New Drugs30, 916.
Li, L., et al. 2010. Cancer Res.70, 2445.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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