2170694-05-8
2170694-05-8 structure
- Name: IRAK4-IN-22
- Chemical Name: IRAK4-IN-22
- CAS Number: 2170694-05-8
- Molecular Formula: C28H28FN7O2
- Molecular Weight: 513.57
- Catalog: Signaling Pathways Immunology/Inflammation IRAK
- Create Date: 2022-10-13 22:02:37
- Modify Date: 2024-01-30 22:40:37
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IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].
| Name | IRAK4-IN-22 |
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| Description | IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1]. |
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| Related Catalog | |
| In Vitro | IRAK4-IN-21 (a 4-fold serial dilution from 10 µM; 1 h) decreases the levels of IL-23 (in THP-1 and DC cells), IL-6 (in HUVEC cells) and MIP-1β (in human whole blood)[1]. Cell Viability Assay[1] Cell Line: THP-1, DC cells (are primed with IFN-γ) Concentration: 10 µM (a 4-fold serial dilution from 10 µM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the levels of IL-23 in the supernatant of THP-1 and DC cells with IC50 of 0.10 and 0.11 µM, respectively. Cell Viability Assay[1] Cell Line: HUVEC cells (IL-1β-stimulated) Concentration: 10 µM (a 4-fold serial dilution from 10 µM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the level of IL-6 in the supernatant of HUVEC cells with an IC50 of 0.11 µM. Cell Viability Assay[1] Cell Line: Human whole blood (IL-1β-stimulated) Concentration: 10 µM (a 4-fold serial dilution from 10 µM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the level of MIP-1β in the human whole blood with an IC50 of 0.51 µM. |
| In Vivo | IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production[1]. Animal Model: BALB/c mice (acute mouse model; IL-1β-stimulated)[1]. Dosage: 75 mg/kg Administration: Oral administration; single (pre-treat). Result: Showed 64% inhibition of IL-6, plasma concentrations was 6817 ng/mL at 0.5 h and 700 ng/mL at 2 h. |
| References |
| Molecular Formula | C28H28FN7O2 |
|---|---|
| Molecular Weight | 513.57 |