2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK STAT
  4. JAK2-IN-13

JAK2-IN-13 is a potent and orally active JAK2 inhibitor with an IC50 of 54.7 nM. JAK2-IN-13 downregulates the expression of p-STAT3 and p-STAT5. JAK2-IN-13 exhibits good bioavailability and potent inhibition of rhEPO-induced extramedullary erythropoiesis and polycythemia vera. JAK2-IN-13 can be used for the study of myeloproliferative neoplasms.

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JAK2-IN-13 Chemical Structure

JAK2-IN-13 Chemical Structure

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JAK2-IN-13 Related Antibodies

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Description

JAK2-IN-13 is a potent and orally active JAK2 inhibitor with an IC50 of 54.7 nM. JAK2-IN-13 downregulates the expression of p-STAT3 and p-STAT5. JAK2-IN-13 exhibits good bioavailability and potent inhibition of rhEPO-induced extramedullary erythropoiesis and polycythemia vera. JAK2-IN-13 can be used for the study of myeloproliferative neoplasms[1].

In Vitro

JAK2-IN-13 (Compound 11) (0.011-25 μM, 72 h) shows potent inhibitory activity against HEL and SET-2 cells, with IC50 values of 0.57 μM and 1.07 μM, respectively[1].
JAK2-IN-13 (0-10 μM, 3 h) significantly inhibits downstream signal pathways of JAK2 and downregulates p-STAT3 and p-STAT5 expression in HEL cells[1].

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

JAK2-IN-13 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEL cells
Concentration: 0, 0.3, 1, 5, 10 μM
Incubation Time: 3 h
Result: Dose-dependent downregulated p-STAT3 and p-STAT5 expression.
Significantly inhibited the phosphorylation of STAT3 and STAT5 at 10 μM for 4 h.
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. T1/2 4.59 h
Mice 5 mg/kg p.o. F 54.8 %
Mice 1 mg/kg i.v. Tmax 2 h
Mice 5 mg/kg p.o. T1/2 4.07 h
Mice 1 mg/kg i.v. Cmax 29.23 ng/mL
Mice 5 mg/kg p.o. Tmax 6 h
Mice 1 mg/kg i.v. AUCinf 166.95 ng·h/mL
Mice 5 mg/kg p.o. Cmax 42.7 ng/mL
Mice 5 mg/kg p.o. AUCinf 457.38 ng·h/mL
In Vivo

JAK2-IN-13 (Compound 11) (50-100 mg/kg, p.o., once daily for 4 days) inhibits rhEPO-induced extramedullary erythropoiesis and polycythemia vera in polycythemia model[1].

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

Animal Model: rhEPO-induced polycythemia model established in female BALB/c mice (8−10 weeks, 17−20 g)[1]
Dosage: 50, 75 and 100 mg/kg
Administration: Oral administration (p.o.), once daily for 4 days
Result: Suppressed the increase in reticulocyte counts and hematocrit expansion induced by rhEPO and alleviated splenomegaly.
Inhibited the expansion of Ter119/CD71 erythroblasts in both the spleen and bone marrow.
Had no significant impact on white blood cell counts and body weight.
Molecular Weight

465.98

Formula

C25H28ClN5O2
SMILES

CC1=CN=C(NC(C=C2)=CC3=C2OCCN4CCCC4)N=C1NC5=CC(Cl)=CC(COC3)=C5
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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JAK2-IN-13 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:

JAK2-IN-13JAKSTATJanus kinaseMyeloproliferative neoplasmsHEL cellsSET-2 cellsBALB/c miceInhibitorinhibitorinhibit

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