2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. JAK Apoptosis Caspase Bcl-2 Family
  4. JAK1/2-IN-3

JAK1/2-IN-3 is a JAK1 and JAK2 inhibitor with IC50 values of 14.73 nM and 10.03 nM, respectively. JAK1/2-IN-3 induces G2/M cell cycle arrest, and induces intrinsic apoptosis via increased Bax and caspase 3/7 levels and reduced Bcl2 expression. JAK1/2-IN-3 can be used for the study of leukemia cancer, breast cancer and colon cancer.

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

JAK1/2-IN-3

JAK1/2-IN-3 Chemical Structure

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JAK1/2-IN-3 Related Antibodies

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Description

JAK1/2-IN-3 is a JAK1 and JAK2 inhibitor with IC50 values of 14.73 nM and 10.03 nM, respectively. JAK1/2-IN-3 induces G2/M cell cycle arrest, and induces intrinsic apoptosis via increased Bax and caspase 3/7 levels and reduced Bcl2 expression. JAK1/2-IN-3 can be used for the study of leukemia cancer, breast cancer and colon cancer[1].

IC50 & Target[1]

JAK1

14.73 nM (IC50)

JAK2

10.03 nM (IC50)

Caspase 3

 

Caspase-7

 

Bax

 

Bcl-2

 

In Vitro

JAK1/2-IN-3 (Compound 3i) inhibits HT-29, MCF-7, HL-60 and HCT-116 cells, with IC50 values of 1.02 μM, 1.87 μM, 7.92 μM and 1.27 μM, respectively. JAK1/2-IN-3 exhibits lower toxicity toward normal WI-38 cells (IC50: 19.93 μM)[1].
JAK1/2-IN-3 (1.02 µM; 24 hours) induces apoptosis in HT-29 cells[1].
JAK1/2-IN-3 (1.02 µM; 24 hours) causes induction of G2/M cell cycle arrest in HT-29 cells[1].
JAK1/2-IN-3 (1.02 µM; 48 hours) increases Bax and caspase 3/7 levels and reduces Bcl2 expression in HT-29 cells[1].

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

JAK1/2-IN-3 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HT-29
Concentration: 1.02 µM
Incubation Time: 24 hours
Result: Significantly increased apoptosis with a 24.39% total apoptosis rate and a 16.9% late apoptotic rate.

Cell Cycle Analysis[1]

Cell Line: HT-29
Concentration: 1.02 µM
Incubation Time: 24 hours
Result: Led to a 5.55-fold increase in the G2/M population compared to the untreated HT-29 cells, accompanied by a notable drop in the G0/G1 and S phase populations by around 24.4 % and 38.6 %, respectively.

RT-PCR[1]

Cell Line: HT-29
Concentration: 1.02 µM
Incubation Time: 48 hours
Result: Showed a 3.34-fold upregulation of Bax, a 0.26-fold downregulation of Bcl2, and 5.96-fold and 9.00-fold increases in caspase-3 and caspase-7, respectively.
Molecular Weight

498.28

Formula

C22H13Cl2N5O5
SMILES

O=C(N(C1=CC=CC=C1)N=C/2NC3=CC=C(Cl)C([N+]([O-])=O)=C3)C2=C\C4=CC=C(Cl)C([N+]([O-])=O)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JAK1/2-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JAK1/2-IN-3JAKApoptosisCaspaseBcl-2 FamilyJanus kinaseMolecular modellingBax/Bcl2Anticancer activity3D-QSARJAK1/2 inhibitorsPhenylpyrazoloneCaspase 3/7DFTInhibitorinhibitorinhibit

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