2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK STAT
  4. JAK2-IN-15

JAK2-IN-15 is an orally active, potent, selective JAK2 inhibitor (IC50 = 1.17 nM). JAK2-IN-15 can inhibit the AK2-STAT signaling pathway. JAK2-IN-15 significantly improves key pathological indicators such as hematocrit and splenomegaly in an Epoetin beta (HY-114134) (rhEPO)-induced mouse model. JAK2-IN-15 can be used for the study of Polycythemia Vera (PV).

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JAK2-IN-15

JAK2-IN-15 Chemical Structure

CAS No. : 3094174-82-7

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JAK2-IN-15 Related Antibodies

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Description

JAK2-IN-15 is an orally active, potent, selective JAK2 inhibitor (IC50 = 1.17 nM). JAK2-IN-15 can inhibit the AK2-STAT signaling pathway. JAK2-IN-15 significantly improves key pathological indicators such as hematocrit and splenomegaly in an Epoetin beta (HY-114134) (rhEPO)-induced mouse model. JAK2-IN-15 can be used for the study of Polycythemia Vera (PV)[1].

IC50 & Target

JAK2

1.17 nM (IC50)

In Vitro

JAK2-IN-15 (Compound 2) exhibits potent JAK2 inhibition (IC50 = 1.17 nM)[1].
JAK2-IN-15 (72 h) effectively inhibits the proliferation of HEL (IC50 = 1.88 μM) and SET-2 (IC50 = 9.56 μM) cells carrying the JAK2V617F mutation[1].
JAK2-IN-15 (0.3-10 μM, 72 h) exhibits significant antiproliferative activities against HEL and SET-2 cells with JAK2V617F mutant by inhibiting the JAK2-STAT signaling pathway in a dose-dependent manner[1].
JAK2-IN-15 (100 μM) inhibits only 17 wild-type kinases, exhibiting strong selectivity[1].

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

JAK2-IN-15 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEL 92.1.7 cells, SET-2
Concentration: 0.3 μM, 1 μM, 3 μM, 10 μM
Incubation Time: 4 h
Result: Effectively inhibited phosphorylation of JAK2 (Y1007/8 site), STAT3, STAT5, AKT and ERK.
In Vivo

JAK2-IN-15 (Compound 2) (25-75 mg/kg, p.o., once daily for 4 days) demonstrates significant therapeutic efficacy in a mouse model of rhEPO-induced polycythemia, dose-dependently inhibiting splenomegaly, hematocrit, and reticulocytosis, with a good safety profile[1].

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

Animal Model: A model of polycythemia and splenomegaly was created using female BALB/c mice (8-10 weeks old, weighing 17-20 g) by subcutaneous injection of 10 units of recombinant human erythropoietin (rhEPO) daily for 4 consecutive days[1].
Dosage: 25 mg/kg, 50 mg/kg, 75 mg/kg
Administration: P.o., once daily for 4 days
Result: Spleen weight decreased.
Dose-dependent inhibition of hematocrit.
Reduction of rhEPO-induced reticulocyte proliferation.
Inhibition of Ter119/CD71 erythroblast expansion in the spleen and bone marrow.
No significant effect on white blood cell count or body weight.
Molecular Weight

517.62

Formula

C29H35N5O4
CAS No.
SMILES

CC1=C2N=C(NC3=CC=C(C(COC/C=C/COCC4=CC=CC(N2)=C4)=C3)OCCN5CCOCC5)N=C1
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-15 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-153094174-82-7JAKSTATJanus kinaseMacrocyclic compoundsDeep learning modelsDrug designCycleGPTInhibitorinhibitorinhibit

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