2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Proteasome NOD-like Receptor (NLR)
  4. NIC-0102

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.

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

NIC-0102 Chemical Structure

NIC-0102 Chemical Structure

CAS No. : 2806031-94-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 336 In-stock
Solution
10 mM * 1 mL in DMSO USD 336 In-stock
Solid
5 mg USD 365 In-stock
10 mg USD 620 In-stock
25 mg USD 1300 In-stock
50 mg USD 2200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

NIC-0102 Related Antibodies

Top Publications Citing Use of Products

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NLRP3 NLRP1 NOD1 NOD2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

proteasom β5

3.7 nM (IC50)

proteasom β2

100.5 nM (IC50)

proteasom β1

113.6 nM (IC50)

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.

NIC-0102 Related Antibodies

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)
T1/2 (h) 4.73 8.36
Tmax (h) 0.08 0.25
Cmax (ng/mL) 376.6 207.7
AUC0-∞ (h•ng/mL) 448.8 489.2
MRT0-∞ (h) 6.14 -
Vz (L/kg) 7.7 -
CL (mL/min/kg) 18.8 -
F (%) - 48.1%
Molecular Weight

418.24

Formula

C21H25BF2N2O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3910 mL 11.9549 mL 23.9097 mL
5 mM 0.4782 mL 2.3910 mL 4.7819 mL
View the Complete Stock Solution Preparation Table

* 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.

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  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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NIC-0102 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NIC-01022806031-94-5NIC0102NIC 0102ProteasomeNOD-like Receptor (NLR)ulcerative colitisJ774A.1BMDMsNLRP3IL-1βASCInhibitorinhibitorinhibit

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