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Cat. No.: HY-187220

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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.

For research use only. We do not sell to patients.

CAS No.: 3119216-05-3
Formula: C₃₃H₄₆N₄O₁₂
Molecular Weight:690.74

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

β5i-IN-2 Chemical Structure

CAS No.: 3119216-05-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

β5i

0.08 μM (IC₅₀)

All Interleukin Related Isoforms :

All TNF Receptor Isoforms :

All JNK Isoforms :

All ERK Isoforms :

All NF-κB Isoforms :

In Vitro

OthersCytokines & ChemokinesInnate Immunity

Others

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].

Cytokines & Chemokines

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].

Innate Immunity

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.

Real Time qPCR^[1]

Cell Line:

RAW 264.7 murine macrophage cells
Concentration:

10, 20, 40 nM
Incubation Time:

1 h (pretreatment); 24 h (stimulation)
Result:

Concentration-dependently reduced IL-1β, IL-6 and TNF-α mRNA expression.

Western Blot Analysis^[1]

Cell Line:

RAW 264.7 murine macrophage cells
Concentration:

10, 20, 40 nM
Incubation Time:

4 h (pretreatment); 15 min (stimulation)
Result:

Reduced p-JNK and p-ERK levels and increased IκBα protein levels, with the strongest effects at 40 nM.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	T_max	AUC_0-t	Bioavailability
Rat^[1]	1.0 mg/kg	i.v.	0.17 h	462 ng/mL	0.083 h	131 ng·h/mL	/
Rat^[1]	10.0 mg/kg	i.g.	0.92 h	32 ng/mL	0.50 h	60 ng·h/mL	4.5 %

In Vivo

β5i-IN-2 (compound ent-F10) (2.5-10.0 mg/kg; p.o.; once daily; 14 days) dose-dependently inhibits arthritis progression in the CIA rat model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (SD) rats (rheumatoid arthritis CIA model, arthritis index ≥2 at study start)^[1]
Dosage:

2.5 mg/kg; 5.0 mg/kg; 10.0 mg/kg
Administration:

p.o.; once daily; 14 days
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.

Related Protocols :

Chemical Information

CAS No. 3119216-05-3
Molecular Weight 690.74
Formula C₃₃H₄₆N₄O₁₂
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
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

Handling Instructions (2659 KB)

References

[1]. Ye X, et al. Discovery of an oral, potent and highly selective immunoproteasome inhibitor for the treatment of rheumatoid arthritis and ulcerative colitis. European journal of medicinal chemistry. 2026 Jul 09;317:119137. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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β5i-IN-2

All Interleukin Related Isoforms

All TNF Receptor Isoforms

All JNK Isoforms

All ERK Isoforms

All NF-κB Isoforms