2. PI3K/Akt/mTOR Immunology/Inflammation
  3. PIKfyve Interleukin Related MHC
  4. 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.

AS2677131

AS2677131 Chemical Structure

CAS No. : 2171502-44-4

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AS2677131 Related Antibodies

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MHC I MHC II

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Description

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[1].

IC50 & Target[1]

IL-12

 

IL-1β

 

IL-6

 

MHC II

 

In Vitro

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.

AS2677131 Related Antibodies

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 100 nM
Incubation Time: 2 h
Result: Reduced p-Akt levels.
In Vivo

AS2677131 (1-30 mg/kg, p.o.) decreases the plasma levels of IL-12p40, IL-6, and TNFα in rats treated with Poly (I:C) (HY-107202) and MDP (HY-127090)[1].
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.

Animal Model: Rats with adjuvant-induced arthritis[1]
Dosage: 1, 3 and 10 mg/kg
Administration: Orally administration, daily for 24 days
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.
Molecular Weight

470.57

Formula

C27H30N6O2
CAS No.
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
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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AS2677131 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:

AS26771312171502-44-4AS 2677131AS-2677131PIKfyveInterleukin RelatedMHCFYVE domain-containing phosphatidylinositol 3-phosphate 5-kinasePhosphatidylinositol 3-phosphate 5-kinaseFab1ILMajor Histocompatibility ComplexIL-12p40IL-6IL-1βc-RelMHC class IIB cellsArthritisInhibitorinhibitorinhibit

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