2. PROTAC Cell Cycle/DNA Damage Immunology/Inflammation
  3. Molecular Glues NEKs NOD-like Receptor (NLR) Interleukin Related
  4. NK7-902 diTFA

NK7-902 diTFA is a selective and orally active CRBN-dependent NEK7 molecular glue degrader with Kd values of 1.5 and 2.6 μM for hNEK7 and mNEK7. NK7-902 diTFA fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 diTFA shows activity in murine systems and induces a profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation. NK7-902 diTFA can be used for the research of inflammation, such as cryopyrin-associated periodic syndromes.

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

NK7-902 diTFA

NK7-902 diTFA Chemical Structure

Size Price Stock Quantity
5 mg In-stock
10 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

NK7-902 diTFA Related Antibodies

Top Publications Citing Use of Products

View All NEKs Isoform Specific Products:

View All Isoforms
NEK1 NEK2 NEK4 NEK6 NEK7

View All NOD-like Receptor (NLR) Isoform Specific Products:

View All Isoforms
NLRP3 NLRP1 NOD1 NOD2

View All Interleukin Related Isoform Specific Products:

View All Isoforms
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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NK7-902 diTFA is a selective and orally active CRBN-dependent NEK7 molecular glue degrader with Kd values of 1.5 and 2.6 μM for hNEK7 and mNEK7. NK7-902 diTFA fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 diTFA shows activity in murine systems and induces a profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation. NK7-902 diTFA can be used for the research of inflammation, such as cryopyrin-associated periodic syndromes[1].

IC50 & Target[1]

NEK7

 

NLRP3 inflammasome

 

IL-1β

 

In Vitro

NK7-902 diTFA (0.005-10000 nM; 18 h pre-treatment) potently and selectively degrades NEK7 (DC50 = 0.2 nM) in human primary monocytes, with partial, stimulus-dependent inhibition of NLRP3 inflammasome-mediated IL-1β secretion[1].
NK7-902 diTFA (0.009-10000 nM; 18 h) potently degrades NEK7 (DC50 = 1.6 nM) in human PBMCs, with full NLRP3 inflammasome inhibition in most CAPS mutations but partial inhibition in the NEK7T348M mutation[1].
NK7-902 diTFA (0.001-10000 nM; 18 h) potently degrades NEK7 in human whole blood (DC50 = 8.7 nM) and neutrophils, with partial IL-1β inhibition in whole blood but full inhibition in isolated neutrophils[1].
NK7-902 diTFA (1-10000 nM; 18 h) potently degrades NEK7 (DC50 = 54.2 nM) in mouse primary splenocytes in a CRBN-dependent manner[1].
NK7-902 diTFA (0.1-10000 nM; 18 h) potently degrades NEK7 (DC50 = 4.1 nM) in NHP blood in vitro[1].
NK7-902 diTFA (20-411 μg/mL; 96 h) degrades NEK7 in human primary blood lymphocytes without inducing significant chromosomal damage or cell cycle delay[1].

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

NK7-902 diTFA Related Antibodies

Western Blot Analysis[1]

Cell Line: Human primary monocytes
Concentration: 0.005, 0.026, 0.13, 0.64, 3.2, 16, 80, 40, 2000, 10000 nM
Incubation Time: 18 h pre-treatment
Result: Induced a dose-dependently NEK7 degradation with DC50 of 0.2 nM and Dmax of >95%.
In Vivo

NK7-902 diTFA (30-300 mg/kg; p.o.; single dose; 6h/16h pre-LPS (HY-D1056) challenge) induces dose-dependent NEK7 degradation and corresponding inhibition of NLRP3 inflammasome-mediated IL-1β release in a mouse acute peritonitis model[1].
NK7-902 diTFA (300 mg/kg; p.o.; single dose; 16h pre-LPS challenge) induces robust NEK7 degradation and significant inhibition of NLRP3 inflammasome-mediated IL-1β release in a mouse CAPS model[1].
NK7-902 diTFA (0.2-2 mg/kg; p.o.; single dose) induces profound, long-lasting NEK7 degradation but only transient IL-1β inhibition in non-human primates[1].

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

Animal Model: Acute peritonitis C57BL/6JRj mice (female, 7-8 weeks old)[1]
Dosage: 30 mg/kg; 100 mg/kg; 300 mg/kg
Administration: P.o.; single dose; 6h pre-LPS challenge; 16h pre-LPS challenge
Result: Induced dose-dependent NEK7 degradation in mouse spleen, with maximum degradation observed at the 300 mg/kg dose at the 8h + 15min time point.
Showed slight recovery of NEK7 protein levels at the 18h + 15min time point.
Accompanied dose-dependent inhibition of IL-1β release in peritoneal lavage fluid.
Molecular Weight

638.51

Formula

C26H28F6N4O8
Appearance

Solid

Color

Light yellow to yellow

SMILES

CCN[C@@H]1CC[C@@H]2N(C3=CC=C(C(N(C4CCC(NC4=O)=O)C5=O)=O)C5=C3)[C@H]1CC2.OC(C(F)(F)F)=O.OC(C(F)(F)F)=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 (156.61 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 1.5661 mL 7.8307 mL 15.6615 mL
5 mM 0.3132 mL 1.5661 mL 3.1323 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (3.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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 1.5661 mL 7.8307 mL 15.6615 mL 39.1537 mL
5 mM 0.3132 mL 1.5661 mL 3.1323 mL 7.8307 mL
10 mM 0.1566 mL 0.7831 mL 1.5661 mL 3.9154 mL
15 mM 0.1044 mL 0.5220 mL 1.0441 mL 2.6102 mL
20 mM 0.0783 mL 0.3915 mL 0.7831 mL 1.9577 mL
25 mM 0.0626 mL 0.3132 mL 0.6265 mL 1.5661 mL
30 mM 0.0522 mL 0.2610 mL 0.5220 mL 1.3051 mL
40 mM 0.0392 mL 0.1958 mL 0.3915 mL 0.9788 mL
50 mM 0.0313 mL 0.1566 mL 0.3132 mL 0.7831 mL
60 mM 0.0261 mL 0.1305 mL 0.2610 mL 0.6526 mL
80 mM 0.0196 mL 0.0979 mL 0.1958 mL 0.4894 mL
100 mM 0.0157 mL 0.0783 mL 0.1566 mL 0.3915 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

NK7-902 diTFA 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:

NK7-902 diTFAMolecular GluesNEKsNOD-like Receptor (NLR)Interleukin RelatedNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesILCRBN molecular glueNEK7NLRP3-dependent IL-1βInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NK7-902 diTFA
Cat. No.:
HY-173154B
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.