β5i-IN-2
β5i-IN-2 is a potent, selective, and orally active inhibitor of the immunoproteasome β5i subunit, with an IC50 of 0.08 μM against human β5i. β5i-IN-2 inhibits LPS (HY-D1056)- and IFN-γ-induced expression of IL-1β, IL-6, and TNF-α, and suppresses the JNK, ERK, and NF-κB signaling pathways. β5i-IN-2 can be used in research related to rheumatoid arthritis and ulcerative colitis.
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- CAS No.: 3119216-05-3
- 화학식: C33H46N4O12
- 분자량:690.74
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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β5i 0.08 μM (IC50) |
β5i-IN-2 (compound ent-F10) (1 μM; serial dilutions; 10-15 min) potently and selectively inhibits the immunoproteasome β5i in cell-free lysate and purified proteasome assays, with an IC50 of 0.08 μM, and a selectivity index of 123.8 over the constitutive proteasome β5[1].
β5i-IN-2 exhibits low affinity for hERG ion channels in HEK293 cells, indicating a low risk of cardiotoxicity[1].
β5i-IN-2 (10-40 nM; pre-treatment for 1 h) reduces the mRNA expression of IL-1β, IL-6 and TNF-α in RAW 264.7 cells in a concentration-dependent manner after stimulation with LPS (100 ng/mL) and IFN-γ (20 ng/mL) for 24 h[1].
β5i-IN-2 (10-40 nM; 4 h pre-treatment) reduces JNK and ERK phosphorylation in RAW 264.7 cells in a concentration-dependent manner following 15 min of stimulation with LPS and IFN-γ, and restores IκBα protein levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 murine macrophage cells
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Concentration:10, 20, 40 nM
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Incubation Time:1 h (pretreatment); 24 h (stimulation)
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Result:Concentration-dependently reduced IL-1β, IL-6 and TNF-α mRNA expression.
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Cell Line:RAW 264.7 murine macrophage cells
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Concentration:10, 20, 40 nM
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Incubation Time:4 h (pretreatment); 15 min (stimulation)
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Result:Reduced p-JNK and p-ERK levels and increased IκBα protein levels, with the strongest effects at 40 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats (rheumatoid arthritis CIA model, arthritis index ≥2 at study start)[1]
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Dosage:2.5 mg/kg; 5.0 mg/kg; 10.0 mg/kg
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Administration:p.o.; once daily; 14 days
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Result:Dose-dependently reduced arthritis progression.
Day-14 arthritis index values were 7.13, 5.25, and 4.75 at 2.5, 5, and 10 mg/kg, respectively.
Produced paw-swelling inhibition rates of 17.2%, 32.3%, and 48.4%, respectively, on day 14, without significant body-weight loss.
Chemical Information
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CAS No. 3119216-05-3
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분자량 690.74
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화학식 C33H46N4O12
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SMILES
O=C(N[C@@H](C)C(N[C@H](C(N[C@@H](C/C=C(C)/C)C([C@@]1(C)CO1)=O)=O)[C@H](O)C2=CC=C(OC)C=C2)=O)CN3CCOCC3.OC(/C=C\C(O)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
β5i-IN-2 Related Classifications
HY-187220 Related Classifications
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