JAK2-IN-21
JAK2-IN-21 is a Janus kinase 2 (JAK2) inhibitor with an IC50 of 12.25 nM. JAK2-IN-21 inhibits the JAK2/STAT3/STAT5 tumor-promoting signaling pathway and reduces JAK2 protein expression. JAK2-IN-21 exhibits selective cytotoxicity against HPV-positive cancer cells and induces cancer cell apoptosis. JAK2-IN-21 can be used in the research of HPV-positive cervical cancer.
For research use only. We do not sell to patients.
- CAS No.: 3038340-43-8
- Formula: C25H19NO4
- Molecular Weight:397.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
JAK2 12.25 nM (IC50) |
STAT3 |
STAT5 |
In Vitro
JAK2-IN-21 (Compound 2q) (48 h) selectively inhibits the viability of HeLa cervical cancer cells with an IC50 of 19.63 μM, while it shows low toxicity to L929 normal fibroblasts with an IC50 of 64.51 μM[1].
JAK2-IN-21 (19.63 μM; 48 h) induces apoptosis in HeLa cervical cancer cells, with a total apoptosis rate of 24.31% after 48 h of treatment at its IC50 concentration[1].
JAK2-IN-21 (19.63-39.26 μM; 24-48 h) inhibits the protein expression of JAK2, STAT3 and STAT5 in HeLa cervical cancer cells in a dose- and time-dependent manner. After treatment at a concentration of 2× its IC50 for 48 h, the level of JAK2 is reduced by up to 98.12%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:19.63 μM
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Incubation Time:48 h
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Result:Induced total apoptosis in 24.31% of HeLa cells, a level comparable to ruxolitinib (34.60% total apoptosis).
Showed a higher proportion of early apoptotic cells relative to late apoptotic cells.
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Cell Line:HeLa cells
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Concentration:19.63 μM (1× IC50); 39.26 μM (2× IC50)
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Incubation Time:24 h; 48 h
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Result:Suppressed JAK2, STAT3, and STAT5 protein levels in a dose- and time-dependent manner.
Reduced JAK2 expression by 27.54% at 1× IC50 for 24 h.
Reduced JAK2 expression by 78.96% at 1× IC50 for 48 h.
Reduced JAK2 expression by 98.12% at 2× IC50 for 48 h.
Showed pronounced inhibition of STAT3 and STAT5 proteins, consistent with suppression of the JAK2/STAT3/STAT5 pro-tumorigenic pathway.
- RNA extraction experimental
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Protocol For Protein Expression And Purification
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 3038340-43-8
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Molecular Weight 397.42
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Formula C25H19NO4
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SMILES
O=C(C1=CC=CC=C1)C2=C(O)C(NC(C3=CC=CC=C3)=O)=CC4=CC=C(OC)C=C42
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)