WEHI-345

WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC 50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulationIn VitroWEHI-345 (500 nM; Raw 267.4 cells) is able to inhibit MDP-induced autophosphorylation activity of RIPK2 in cells. WEHI-345 (500 nM; 0 hour, 2 hours, 4 hours, 8 hours; BMDMs or THP-1 cells) potently blocks MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in bone marrow-derived macrophages (BMDMs). In THP-1 cells, WEHI-345 reduces mRNA levels of NF-kB targets such as TNF, IL-8, IL-1b and A20. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Raw 267.4 cells Concentration: 500 nM Incubation Time: Result: Inhibited MDP-induced autophosphorylation activity of RIPK2 in cells. RT-PCRCell Line: BMDMs or THP-1 cells Concentration: 500 nM Incubation Time: 0 hour, 2 hours, 4 hours, 8 hours Result: Blocked MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in BMDMs. And reduced mRNA levels of NF-kB targets in THP-1 cells.In VivoWEHI-345 (20 mg/kg; intraperitoneal injection; twice daily; for 6 days; C57BL/6 male mice) treatment reduces disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improves body weight and reduces cytokine and chemokine levels, indicating an overall improvement of the condition in experimental autoimmune encephalomyelitis (EAE)-induced wild-type C57Bl/6 mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 male mice (8-week-old) Dosage: 20 mg/kg Administration: Intraperitoneal injection; twice daily; for 6 days Result: Reduced disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improved body weight and reduced cytokine and chemokine levels.Form:SolidIC50& Target:IC 50 : 0.13 μM (RIPK2 kinase)

Specifications & Purity: WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC 50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulationIn VitroWEHI-345 (500 nM; Raw 267.4 cells) is able to inhibit MDP-induced autophosphorylation activity of RIPK2 in cells. WEHI-345 (500 nM; 0 hour, 2 hours, 4 hours, 8 hours; BMDMs or THP-1 cells) potently blocks MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in bone marrow-derived macrophages (BMDMs). In THP-1 cells, WEHI-345 reduces mRNA levels of NF-kB targets such as TNF, IL-8, IL-1b and A20. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Raw 267.4 cells Concentration: 500 nM Incubation Time: Result: Inhibited MDP-induced autophosphorylation activity of RIPK2 in cells. RT-PCRCell Line: BMDMs or THP-1 cells Concentration: 500 nM Incubation Time: 0 hour, 2 hours, 4 hours, 8 hours Result: Blocked MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in BMDMs. And reduced mRNA levels of NF-kB targets in THP-1 cells.In VivoWEHI-345 (20 mg/kg; intraperitoneal injection; twice daily; for 6 days; C57BL/6 male mice) treatment reduces disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improves body weight and reduces cytokine and chemokine levels, indicating an overall improvement of the condition in experimental autoimmune encephalomyelitis (EAE)-induced wild-type C57Bl/6 mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 male mice (8-week-old) Dosage: 20 mg/kg Administration: Intraperitoneal injection; twice daily; for 6 days Result: Reduced disease score, inflammatory infiltrate, histological score and recruitment of dendritic cells to the site of inflammation. And improved body weight and reduced cytokine and chemokine levels.Form:SolidIC50& Target:IC 50 : 0.13 μM (RIPK2 kinase)

Grade: Moligand™

Molecular Formula: C22H23N7O

Molecular Weight: 401.46

PubChem CID: 56602554

Isomeric SMILES: CC1=CC=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)(C)CNC(=O)C4=CC=NC=C4

Storage Temperature: Protected from light;Store at -20°C;Argon charged

Shipped in: Ice chest + Ice pads

UPC:

51373401

Weight:

1.06 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

W651350-25mg

Country of Origin:

China

CAS:

1354825-58-3

Product Size:

25mg

Harmonized Tariff Code:

2931.90.90