2. Immunology/Inflammation Cell Cycle/DNA Damage
  3. NOD-like Receptor (NLR) Interleukin Related NEKs
  4. NLRP3-IN-79

NLRP3-IN-79 is an orally active NLRP3 inhibitor. NLRP3-IN-79 inhibits NLRP3 inflammasome with an IC50 of 10.69 nM. NLRP3-IN-79 blocks NLRP3 inflammasome assembly by directly binding to NLRP3 and disrupting the NEK7-NLRP3 interaction. NLRP3-IN-79 can be used for the study of NLRP3-driven diseases model, including systemic inflammation, peritonitis, and colitis.

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NLRP3-IN-79

NLRP3-IN-79 Chemical Structure

CAS No. : 3088796-72-6

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

NLRP3-IN-79 Related Antibodies

Top Publications Citing Use of Products

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NLRP3 NLRP1 NOD1 NOD2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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NEK1 NEK2 NEK4 NEK6 NEK7

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Description

NLRP3-IN-79 is an orally active NLRP3 inhibitor. NLRP3-IN-79 inhibits NLRP3 inflammasome with an IC50 of 10.69 nM. NLRP3-IN-79 blocks NLRP3 inflammasome assembly by directly binding to NLRP3 and disrupting the NEK7-NLRP3 interaction. NLRP3-IN-79 can be used for the study of NLRP3-driven diseases model, including systemic inflammation, peritonitis, and colitis[1].

IC50 & Target[1]

NLRP3 inflammasome

10.69 nM (IC50)

NEK7

 

IL-18

 

IL-1β

 

In Vitro

NLRP3-IN-79 (compound B6) (3-30 nM, 5 h 45 min) inhibits activation and assembly of NLRP3 inflammasome in Lipopolysaccharide (LPS) (HY-D1056) (100 ng/mL, 4 h) + Adenosine triphosphate (ATP) (HY-B2176) (5 mM, 45 min) induced human and bone macrophages[1].
NLRP3-IN-79 (3-30 nM, 1 h) blocks NLRP3 inflammasome assembly by disrupting NEK7-NLRP3 interaction in LPS (100 ng/mL, 4 h) + ATP (5 mM, 45 min) induced BMDMs[1].
NLRP3-IN-79 (0-500 μM, 20 h) has no significant hepatocellular toxicity in AML-12 and HL-7702[1].

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

NLRP3-IN-79 Related Antibodies

Western Blot Analysis[1]

Cell Line: LPS + ATP induced HMDMs and BMDMs
Concentration: 3, 10, and 30 nM was applied to LPS-primed (100 ng/mL, 4 h) prior to ATP stimulation (5 mM, 45 min)
Incubation Time: 5 h 45 min
Result: Markedly reduced the caspase-1 cleavage and IL-1β maturation.
Reduced secretion of IL-1β and IL-18.
Markedly reduced the caspase-1 cleavage and IL-1β maturation triggered by both nigericin and monosodium urate.
Reduced secretion of IL-1β and IL-18.
Inhibited formation of NLRP3/ASC/Pro-caspase-1 complexes.

Western Blot Analysis[1]

Cell Line: LPS + ATP induced BMDMs
Concentration: 3, 10, and 30 nM was applied to LPS-primed (100 ng/mL, 4 h) prior to ATP stimulation (5 mM, 45 min)
Incubation Time: 5 h 45 min
Result: Attenuated ATP-induced ASC oligomerization.
Disrupted the interaction of NEK7-NLRP3 in a concentration-dependent manner.
In Vivo

NLRP3-IN-79 (compound B6) (5-20 mg/kg, i.p., once) ameliorates LPS-induced systemic inflammation in C57BL/6 mice[1].
NLRP3-IN-79 (5-20 mg/kg, i.p., once) mitigates Monosodium urate (MSU) (HY-B2130A)-induced peritonitis in C57BL/6 mice[1].
NLRP3-IN-79 (5-20 mg/kg, o.p., 10 days) markedly alleviates Dextran sulfate sodium salt (DSS) (HY-116282C)-induced colitis in female C57BL/6 mice[1].

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

Animal Model: LPS (20 mg/kg, i.p., once) induced inflammatory model in female C57BL/6 mice (6-8 weeks, 18-20 g)[1].
Dosage: 5, 10, 20 mg/kg
Administration: i.p., 1 h before LPS administration, blood samples were collected for detecting 2 h after LPS administration.
Result: Reduced IL-1β production in both serum and peritoneal lavage fluid.
Reduced proportion of neutrophils in the peritoneal lavage fluids.
Ameliorated LPS-induced systemic inflammation in mice.
Animal Model: MSU (30 mg/kg, i.p., once) induced inflammatory mode in female C57BL/6 mice (6-8 weeks, 18-20 g)[1].
Dosage: 5; 10; 20 mg/kg
Administration: i.p., before MSU induction.
Result: Inhibited infiltration of neutrophils in the peritoneal lavage fluid.
Animal Model: DSS (2.8%, p.o., 10 days) induced inflammatory model in female C57BL/6 mice (6-8 weeks old, 18-20 g)[1].
Dosage: 5, 10, 20 mg/kg
Administration: i.p., for 10 consecutive days.
Result: Inhibited infiltration of neutrophils in the peritoneal lavage fluid.
Molecular Weight

392.49

Formula

C23H28N4O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CCNC(N(CC1=CN=CC=C1)CC(NC2=C3C(CCC3)=CC4=C2CCC4)=O)=O
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 (254.78 mM; ultrasonic and warming and heat to 60°C; 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 2.5478 mL 12.7392 mL 25.4784 mL
5 mM 0.5096 mL 2.5478 mL 5.0957 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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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 2.5478 mL 12.7392 mL 25.4784 mL 63.6959 mL
5 mM 0.5096 mL 2.5478 mL 5.0957 mL 12.7392 mL
10 mM 0.2548 mL 1.2739 mL 2.5478 mL 6.3696 mL
15 mM 0.1699 mL 0.8493 mL 1.6986 mL 4.2464 mL
20 mM 0.1274 mL 0.6370 mL 1.2739 mL 3.1848 mL
25 mM 0.1019 mL 0.5096 mL 1.0191 mL 2.5478 mL
30 mM 0.0849 mL 0.4246 mL 0.8493 mL 2.1232 mL
40 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5924 mL
50 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2739 mL
60 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0616 mL
80 mM 0.0318 mL 0.1592 mL 0.3185 mL 0.7962 mL
100 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
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NLRP3-IN-79 Related Classifications

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  • 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:

NLRP3-IN-793088796-72-6NOD-like Receptor (NLR)Interleukin RelatedNEKsILNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesNLRP3 inflammasomeNEK7-NLRP3systemic inflammationperitonitisand colitisInhibitorinhibitorinhibit

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