Art. -Nr.: HY-151252

NIC-0102

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NIC-0102 is an orally active proteasome inhibitor (pIC₅₀=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.

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Reinheit: 98.79%
CAS. Nr.: 2806031-94-5
Formel: C₂₁H₂₅BF₂N₂O₄
Molecular Weight:418.24

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

NIC-0102 Chemical Structure

CAS. Nr.: 2806031-94-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

proteasom β5

3.7 nM (IC₅₀)

proteasom β2

100.5 nM (IC₅₀)

proteasom β1

113.6 nM (IC₅₀)

Alle NOD-like Receptor (NLR) Isoform-spezifische Produkte anzeigen :

In Vitro

NIC-0102 (compound 27) (7.5, 15, 30, 60 nM; 1h) specifically suppresses NLRP3 inflammasome activation in LPS-primed J774A.1 and BMDM cells^[1].
NIC-0102 (7.5, 15, 30, 60 nM; 1h) induces polyubiquitination of NLRP3 via inhibition of the proteasome during the activation step in LPS-primed J774A.1 cells^[1].
NIC-0102 (7.5, 15, 30, 60 nM; 1h) exhibits inhibitory effects on NF-κB in the priming step of the NLRP3 pathway in LPS-primed J774A.1 cells^[1].
NIC-0102 (15, 60 nM; 1h) blocks NLRP3-ASC interaction and ASC oligomerization in LPS-primed J774A.1 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

J774A.1 and BMDM cells (LPS-primed)
Concentration:

7.5, 15, 30, 60 nM
Incubation Time:

1 h
Result:

Inhibited the release of IL-1β in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

J774A.1 cells (LPS-primed)
Concentration:

7.5, 15, 30, 60 nM
Incubation Time:

1 h
Result:

Dose-dependently inhibited the release of mature IL-1β and the caspase-1 p20 subunit in supernatants from J774A.1 cells but did not affect pro-IL-1β, pro-caspase-1, NLRP3, or ASC in cell lysates.
Increased the polyubiquitinated NLRP3 protein in adose-dependent manner, and significantly increased the amount of c-Cbl and Cbl-b.
Showed an inhibitory effect on the NF-κB subunit p65, phosphorylated p65, and NLRP3 protein at 60 nM, at which NF-κB-dependent TNF-α secretion was slightly decreased.

Western Blot Analysis^[1]

Cell Line:

J774A.1 cells (LPS-primed)
Concentration:

15, 60 nM
Incubation Time:

1 h
Result:

Inhibited the interaction between NLRP3and ASC stimulated by LPS and nigericin.
Showed a concentration-dependent suppression effect on ASC oligomerization.

In Vivo

NIC-0102 (0.125, 0.25, 0.5 mg/kg; p.o.; single every 72 h for 10 days) shows strong protection against DSS-induced acute colitis in mice^[1].

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

Animal Model:

Male C57BL/6 mice (6 to 8-week-old; DSS-induced ulcerative colitis model)^[1].
Dosage:

0.125, 0.25, and 0.5 mg/kg
Administration:

Oral gavage; single every 72 h for 10 days.
Result:

Significantly suppressed weight and fecal occult blood.
Decreased colonic length in a dose-dependent manner.
Resulted in a dose-dependent reduction in tissue-associated IL-1β concentration and significantly inhibited pro-IL-1β.

Animal Model:

Male C57BL/6 mice (6 to 8-week-old)^[1].
Dosage:

0.5 mg/kg (for i.v.); 1 mg/kg (for p.o.)
Administration:

Intravenous injection; Oral gavage; single.

Result:

1.19 Pharmacokinetic Parameters of NIC-0102 in male C57BL/6 mice^[1].

	IV (0.5 mg/kg)	PO (1 mg/kg)
T_1/2 (h)	4.73	8.36
T_max (h)	0.08	0.25
C_max (ng/mL)	376.6	207.7
AUC_0-∞ (h•ng/mL)	448.8	489.2
MRT_0-∞ (h)	6.14	-
V_z (L/kg)	7.7	-
CL (mL/min/kg)	18.8	-
F (%)	-	48.1%

Chemical Information

CAS. Nr. 2806031-94-5
Appearance Solid
Molecular Weight 418.24
Formel C₂₁H₂₅BF₂N₂O₄
Color White to off-white
SMILES

CC(C[C@@H](B(O)O)NC([C@@H](NC(C1=C(C=CC=C1F)F)=O)CC2=CC=CC=C2)=O)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (239.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3910 mL

11.9549 mL

23.9097 mL

5 mM

0.4782 mL

2.3910 mL

4.7819 mL

10 mM

0.2391 mL

1.1955 mL

2.3910 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (5.98 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (5.98 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wu X, et al. Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity. J Med Chem. 2022 Sep 5. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3910 mL	11.9549 mL	23.9097 mL	59.7743 mL
	5 mM	0.4782 mL	2.3910 mL	4.7819 mL	11.9549 mL
	10 mM	0.2391 mL	1.1955 mL	2.3910 mL	5.9774 mL
	15 mM	0.1594 mL	0.7970 mL	1.5940 mL	3.9850 mL
	20 mM	0.1195 mL	0.5977 mL	1.1955 mL	2.9887 mL
	25 mM	0.0956 mL	0.4782 mL	0.9564 mL	2.3910 mL
	30 mM	0.0797 mL	0.3985 mL	0.7970 mL	1.9925 mL
	40 mM	0.0598 mL	0.2989 mL	0.5977 mL	1.4944 mL
	50 mM	0.0478 mL	0.2391 mL	0.4782 mL	1.1955 mL
	60 mM	0.0398 mL	0.1992 mL	0.3985 mL	0.9962 mL
	80 mM	0.0299 mL	0.1494 mL	0.2989 mL	0.7472 mL
	100 mM	0.0239 mL	0.1195 mL	0.2391 mL	0.5977 mL

Keywords

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NIC-0102

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Covalent Screening Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Antidepressant Compound Library

Pain-Related Compound Library

Protease Inhibitor Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Boronic Acid Compound Library

Anti-Hematopathy Compound Library

Inflammasomes related Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Pattern Recognition Receptors Library

Alle NOD-like Receptor (NLR) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NIC-0102

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Covalent Screening Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Antidepressant Compound Library

Pain-Related Compound Library

Protease Inhibitor Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Boronic Acid Compound Library

Anti-Hematopathy Compound Library

Inflammasomes related Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Pattern Recognition Receptors Library

Alle NOD-like Receptor (NLR) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NIC-0102 Related Classifications

HY-151252 Related Classifications