RIPK2 Inhibitor 1, Inhibitor | RIPK2, inhibitor
RIPK2 Inhibitor 1
Synonyms
RIPK2 Inhibitor 1; 3-benzamido-4-methyl-N-[3-(1-methyl-1H-imidazol-2yl)phenyl] benzamide; RIPK2; inhibitor
Form/Format
Powder
Solubility
Stocks should be made up in 100% DMSO to 10-20mM. Stocks can be diluted in >12% DMSO to desired concentration or dissolved in 100% olive oil.
Cell-based Inhibition Kinetics
Left side: Inhibition was carried out for 24-36 hours on Hodgkins lymphoma cell line KMH2 revealing constitutively active RIPK2. This was followed by lysis and immunoprecipitation (IP) with rabbit anti-RIPK2 antibody overnight for total RIPK2 pull down. Following Protein G pull down and wash, 32P-gamma-ATP is added and kinase reaction allowed to proceed for 30 minutes at 30 degree C. Following kinase reaction, SDS-PAGE was used to separate out the proteins, gel was then dried and exposed to film. The p60 RIPK2 band was quantitated.
Right side: NFkappaB gene reporter assay determination of inhibition of MDP stimulated NFkappaB activity. An approximate EC50 determination for inhibition of MDP driven-NFkappaB activation is shown.
RIPK2 Inhibitor 1
In vivo: May be evaluated at 1-15ug/g body weight.
In vivo inhibition of DSS-induced colitis
1a-/-of 1a+/-Wild type Percent Survival Days after 3% DSS addition 1a -/-+ RIPK2 Inhibitor 1 (D3, 5, 7) Add 3% DSS Add WATER 0 5 10 15 20 0 20 40 60 80 100 1a +/-+ RIPK2 Inhibitor 1 (D3, 5, 7)
DSS-induced inflammation can be inhibited by RIPK2 inhibitor 1 at 1ug/g body weight injected intraperitoneally (IP) at day 3, 5 and 7 (during period of active disease and time of recovery). The Kaplan-Meir survival curve is plotted for Rassf 1a-/-and 1a+/-mice. Both potentially have RIPK2 unchecked in colonic tissue (and hence elevated inflammation) if Rassf1a is missing. N = 12-20 animals per condition; p value > 0.001.
In vitro: IC50 is 5-50 nM depending on cell type.
Right side: NFkappaB gene reporter assay determination of inhibition of MDP stimulated NFkappaB activity. An approximate EC50 determination for inhibition of MDP driven-NFkappaB activation is shown.
RIPK2 Inhibitor 1
In vivo: May be evaluated at 1-15ug/g body weight.
In vivo inhibition of DSS-induced colitis
1a-/-of 1a+/-Wild type Percent Survival Days after 3% DSS addition 1a -/-+ RIPK2 Inhibitor 1 (D3, 5, 7) Add 3% DSS Add WATER 0 5 10 15 20 0 20 40 60 80 100 1a +/-+ RIPK2 Inhibitor 1 (D3, 5, 7)
DSS-induced inflammation can be inhibited by RIPK2 inhibitor 1 at 1ug/g body weight injected intraperitoneally (IP) at day 3, 5 and 7 (during period of active disease and time of recovery). The Kaplan-Meir survival curve is plotted for Rassf 1a-/-and 1a+/-mice. Both potentially have RIPK2 unchecked in colonic tissue (and hence elevated inflammation) if Rassf1a is missing. N = 12-20 animals per condition; p value > 0.001.
In vitro: IC50 is 5-50 nM depending on cell type.
Preparation and Storage
Store at -80 degree C in appropriate aliquots to avoid multiple freeze-thaw cycles.
Related Product Information for RIPK2, inhibitor
Background: RIPK2 (Receptor Interacting Protein Kinase 2) is the obligate kinase of the NOD2 intracellular pathogen recognition pathway receptor and an upstream kinase activator for NFkappaB via activation of TAK1. Inhibiting the activity of RIPK2 may be important in controlling inflammatory responses.
Product Categories/Family for RIPK2, inhibitor
References
Salla M et al. Identification and Characterization of Novel Receptor-Interacting Serine/Threonine-Protein Kinase 2 Inhibitors using structural similarity analysis. 2018 J Pharmacol Exp Ther 365: 354-367.
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Product Notes
The RIPK2 (Catalog #AAA191612) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "RIPK2 Inhibitor 1, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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