LU-001i
LU-001i is a highly specific proteasome β1i (LMP2) inhibitor. LU-001i alone has no significant immunomodulatory effect, but when combined with the LMP7 inhibitor (PRN1126), it can exert anti-inflammatory and immunomodulatory effects. LU-001i can be used for the study of autoimmune diseases.
For research use only. We do not sell to patients.
- CAS No.: 1620107-60-9
- Formula: C28H43F2N7O6
- Molecular Weight:611.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Raji | IC50 |
>100 μM
Compound: 37, LU-001i
|
Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
|
[PMID: 25006746] |
| Raji | IC50 |
0.095 μM
Compound: 37, LU-001i
|
Inhibition of proteasome subunit beta-1i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
Inhibition of proteasome subunit beta-1i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
|
[PMID: 25006746] |
| Raji | IC50 |
24 μM
Compound: 37, LU-001i
|
Inhibition of 20s proteasome subunit beta-1c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
Inhibition of 20s proteasome subunit beta-1c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
|
[PMID: 25006746] |
| RPMI-8226 | IC50 |
>100 μM
Compound: 37, LU-001i
|
Inhibition of proteasome subunit beta-2c/i in human RPMI8226 cells by fluorescent densitometry
Inhibition of proteasome subunit beta-2c/i in human RPMI8226 cells by fluorescent densitometry
|
[PMID: 25006746] |
| RPMI-8226 | IC50 |
0.13 μM
Compound: 37, LU-001i
|
Inhibition of proteasome subunit beta-1i in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry
Inhibition of proteasome subunit beta-1i in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry
|
[PMID: 25006746] |
| RPMI-8226 | IC50 |
47 μM
Compound: 37, LU-001i
|
Inhibition of 20s proteasome subunit beta-1c in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry
Inhibition of 20s proteasome subunit beta-1c in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry
|
[PMID: 25006746] |
| RPMI-8226 | IC50 |
65 μM
Compound: 37, LU-001i
|
Inhibition of proteasome subunit beta-5c/i in human RPMI8226 cells by fluorescent densitometry
Inhibition of proteasome subunit beta-5c/i in human RPMI8226 cells by fluorescent densitometry
|
[PMID: 25006746] |
Chemical Information
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CAS No. 1620107-60-9
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Molecular Weight 611.68
-
Formula C28H43F2N7O6
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SMILES
O=C([C@@H]1CC(F)(F)CN1C([C@@H](NC(CN=[N+]=[N-])=O)C)=O)N[C@@H](CCCC)C(N[C@@H](CC2CCCCC2)C([C@]3(C)OC3)=O)=O
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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.
Protocols
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)