JAK-IN-44
JAK-IN-44 is an orally active and selective JAK2 inhibitor, with IC50 values of 0.2 nM, 7.3 nM, 21 nM and 27 nM against JAK2, TYK2, JAK1 and JAK3, respectively. JAK-IN-44 inhibits disease phenotypes in adjuvant-induced arthritis, systemic lupus erythematosus and experimental autoimmune uveitis models, and improves the survival rate of mice in LPS (HY-D1056)-induced sepsis models. JAK-IN-44 can be used in the research of autoimmune and inflammatory diseases such as systemic lupus erythematosus, uveitis, rheumatoid arthritis and sepsis.
For research use only. We do not sell to patients.
- CAS No.: 2119040-02-5
- Formula: C18H21N7O2S
- Molecular Weight:399.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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JAK1 21 nM (IC50) |
JAK2 0.2 nM (IC50) |
JAK3 27 nM (IC50) |
Tyk2 7.3 nM (IC50) |
JAK-IN-44 (compound Ia) inhibits JAK kinase activity, with IC50 values of 21, 0.2, 27, and 7.3 nM against JAK1, JAK2, JAK3, and TYK2, respectively, and exhibits the strongest inhibitory activity against JAK2[2].
JAK-IN-44 exhibits an IC50 of > 30 μM against hERG in automated patch-clamp assays using HEK293 cells stably expressing hERG[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Continuous administration of JAK-IN-44 (30 mg/kg/day for 14 days) to rats causes no obvious toxicity, and no significant differences are observed in various organ tissues and hematological indices compared with the vehicle group; in contrast, Baricitinib (HY-15315) at the same dose induces significant shrinkage of the thymus and spleen[2].
JAK-IN-44 (compound Ia; 10 mg/kg for the first 38 days followed by 22.5 mg/kg; p.o.; BID; 12 weeks) controls the levels of anti-double-stranded DNA IgG autoantibodies in female MRL/MpJ-Faslpr systemic lupus erythematosus mice, with efficacy comparable to that of Baricitinib[1].
JAK-IN-44 (compound Ia; 30 mg/kg; p.o.; BID; administered starting on day 3 post-immunization) reduces the clinical score of uveitis in a female Lewis rat model of experimental autoimmune uveitis induced by bovine IRBP R16, with a particularly pronounced effect in the early stage of the disease, and no significant body weight abnormalities or severe adverse reactions are observed[3].
JAK-IN-44 (90 mg/kg; p.o.; BID; administered starting on day 3 post-immunization) significantly reduces clinical scores in the same experimental autoimmune uveitis model, with no obvious body weight abnormalities or severe adverse effects[3].
JAK-IN-44 (p.o.; BID; 12 weeks) significantly controls proteinuria in MRL/MpJ-Faslpr mice, with efficacy comparable to that of Baricitinib. Moreover, the high-dose group exerts stronger inhibitory effects on autoantibody production, lymph node swelling and skin ulceration than the low-dose group[1].
JAK-IN-44 (compound Ia; 45 mg/kg; p.o.; BID) improves survival in male C57BL/6 mice with LPS-induced sepsis, with a 70% survival rate on day 6, compared with 20% in the vehicle group, which is comparable to the 70% survival rate in the 10 mg/kg dexamethasone group[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MRL/MpJ-Faslpr (female, 7-8 weeks old at dosing; spontaneous systemic lupus erythematosus model); C57BL/6 (negative control)[1]
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Dosage:10 mg/kg for first 38 days; 22.5 mg/kg thereafter
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Administration:p.o.; twice daily; 12 weeks
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Result:Controlled anti-dsDNA IgG levels comparably to Baricitinib and more strongly suppressed lymph-node swelling and skin lesions.
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Animal Model:Rat adjuvant arthritis induced with Mycobacterium tuberculosis H37Ra in paraffin oil[2]
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Dosage:0.5 mg/kg; 1.0 mg/kg; 1.5 mg/kg; 10 mg/kg; 15 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Exhibited disease inhibition rates of 16%, 28%, 50%, 100%, and 100% at doses of 0.5 mg/kg, 1.0 mg/kg, 1.5 mg/kg, 10 mg/kg, and 15 mg/kg, respectively.
Reduced paw volumes to near normal levels at 10 mg/kg and 15 mg/kg.
Confirmed significant inhibition of disease pathology via histopathological and radiological analyses, with reduced inflammatory cell infiltration, connective tissue hyperplasia, and bone proliferation at 10 mg/kg and 15 mg/kg.
Increased body weights more significantly than vehicle control rats.
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Animal Model:Lewis rats (female, 6-8 weeks old, uveitis induced via subcutaneous injection of multi-component emulsion)[3]
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Dosage:30 mg/kg; 90 mg/kg
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Administration:p.o.; twice daily; Day 3 post-induction to Day 16
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Result:Significantly reduced clinical scores versus vehicle, particularly during early disease, without marked body-weight abnormality at 30 mg/kg.
Significantly reduced clinical scores versus vehicle without marked body-weight abnormality at 90 mg/kg.
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Animal Model:C57BL/6 (male, 6-8 weeks old, LPS-induced sepsis)[4]
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Dosage:45 mg/kg
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Administration:p.o.; BID; 6 days
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Result:Achieved a 70% survival rate at day 6 post-LPS injection.
Significantly reduced sepsis-induced mortality compared to the vehicle group (20% survival rate at day 6).
Chemical Information
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CAS No. 2119040-02-5
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Molecular Weight 399.47
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Formula C18H21N7O2S
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SMILES
N#CCC1(CCN(S(=O)(CC)=O)CC1)N2N=CC(C3=C4C=CNC4=NC=N3)=C2
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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)
JAK-IN-44 Related Classifications
HY-188034 Related Classifications
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