1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  2. JAK STAT Apoptosis
  3. 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.

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JAK2-IN-21

JAK2-IN-21 Chemical Structure

CAS No. : 3038340-43-8

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Description

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[1].

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.

Apoptosis Analysis[1]

Cell Line: HeLa cells
Concentration: 19.63 μM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 19.63 μM (1× IC50); 39.26 μM (2× IC50)
Incubation Time: 24 h; 48 h
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.
Molecular Weight

397.42

Formula

C25H19NO4

CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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JAK2-IN-21
Cat. No.:
HY-183670
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