AS2677131
AS2677131 is a potent and orally active PIKfyve inhibitor. AS2677131 inhibits f IL-12p40, IL-6 and IL-1β through a PIKfyve-c-Rel pathway. AS2677131 selectively inhibits DNA-binding activity of c-Rel to IL-12p40 and IL-1β promoter. AS2677131 inhibits MHC class II expression on B cells. AS2677131 can be used for the researches of inflammation and immunology, such as arthritis.
For research use only. We do not sell to patients.
- CAS No.: 2171502-44-4
- Formula: C27H30N6O2
- Molecular Weight:470.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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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IL-12 |
IL-1β |
IL-6 |
MHC II |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
2.4 nM
Compound: 69; AS2677131
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Antiinflammatory activity in mouse RAW264.7 cells assessed as effect on LPS induced IL-12p40 level measured after 24 hrs by RT-qPCR analysis
Antiinflammatory activity in mouse RAW264.7 cells assessed as effect on LPS induced IL-12p40 level measured after 24 hrs by RT-qPCR analysis
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[PMID: 37981443] |
AS2677131 inhibits IL-12p40 production with an IC50 of 2.4 nM and inhibits IL-1β and IL-6 levels in RAW264.7 mouse macrophage cells[1].
AS2677131 (0.1-10000 nM) inhibits IL-12p40 and IL-6 in mouse peritoneal macrophages[1].
AS2677131 (0.1-10000 nM) inhibits IL-12p40 and IL-6 in mouse bone marrow-derived dendritic cells[1].
AS2677131 (10 μM) shows no significant effect on intracellular Ca2+ influx in Ramos cells[1].
AS2677131 (200 nM) inhibits PI (3,5) P2 production by more than 90% in RAW264.7 cells[1].
AS2677131 (100 nM, 2 h) increases the size of RAW264.7 cells and induces numerous small vesicles in the cytoplasm[1].
AS2677131 (10-100 nM, 2h) decreases the promoter activity and inhibits the binding of c-Rel to the promoters of IL-12p40 and IL-1β in RAW264.7 cells[1].
AS2677131 (100 nM, 2 h) reduces p-Akt levels in RAW264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cells
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Concentration:100 nM
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Incubation Time:2 h
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Result:Reduced p-Akt levels.
AS2677131 (1-10 mg/kg, p.o.) reduces the expression of MHC class II molecules on the surface of CD45R+ B cells in rats[1].
AS2677131 (1-10 mg/kg, p.o., daily for 24 days) reduces inflammation in rats with adjuvant-induced arthritis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats with adjuvant-induced arthritis[1]
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Dosage:1, 3 and 10 mg/kg
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Administration:Orally administration, daily for 24 days
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Result:Reduced paw swelling (swelling inhibition rates of 34.3% and 78.3% at doses of 3 and 10 mg/kg, respectively).
Reversed body weight loss.
Decreased joint histological scores (including bone destruction, cartilage destruction, synovial thickening, and inflammatory cell infiltration.
Reduced the proportion of CD3-CD45RA+CD62Llow activated B cells in peripheral blood.
Chemical Information
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CAS No. 2171502-44-4
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Molecular Weight 470.57
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Formula C27H30N6O2
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SMILES
O=C(C1=CC=C(NC(C)=C2CC)C2=N1)NC3=CN=CC(C4=CC=C(N5C[C@@H](C)O[C@@H](C)C5)N=C4)=C3
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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)
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