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WEHI-345 is a potent and selective RIPK2 inhibitor which shows NOD signalling events yet prevents inflammatory cytokine production. WEHI-345 delays RIPK2 ubiquitylation and NF-κB activation downstream of NOD engagement. WEHI-345 proved to be highly specific for RIPK2(Kd=46 nM) and displayed negligible activity (>10 μM) against RIPK1, RIPK4 and RIPK5.
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.
In vivo, WEHI-345 ameliorates experimental autoimmune encephalomyelitis in mice. WEHI-345 also potently inhibited MDP-induced cytokine and chemokine secretion in the mouse macrophage Raw 264.7 cell line. WEHI-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.
Mol Med Rep. 2024 Jan ;36.
Mettl3‑mediated m6A RNA methylation regulates osteolysis induced by titanium particles
WEHI-345 purchased from AbMole
Patent. US2024024368A1 2024-12-19.
Patent. US2024024368A1
WEHI-345 purchased from AbMole
Patent. US2024024368A1 2024 Dec 19; .
Patent. US2024024368A1
WEHI-345 purchased from AbMole
| Molecular Weight | 401.46 |
| Formula | C22H23N7O |
| CAS Number | 1354825-58-3 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related RIPK Products |
|---|
| Necrostatin-1
Necrostatin-1 (NEC-1) is a potent inhibitor of necroptosis, with an EC50 of 490 nM in Jurkat cells. Necrostin-1 is the first identified RIPK1 inhibitor, EC50=182 nM, that reduces inflammation and inhibits colitis associated tumorigenesis. Necrostatin-1 (Nec-1) is also an inhibitor of IDO. |
| GSK481
GSK481 is a highly effective, selective and specific RIPK1 inhibitor with an IC50 value of 1.3 nM, which can inhibit the phosphorylation of Ser166 in wild-type human RIPK1 (IC50 value of 2.8 nM). The IC50 value of GSK481 against U937 cells was 10 nM. |
| GSK583
GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM. |
| Necrostatin-5
Necrostatin-5 is an inhibitor of necroptosis (non-apoptotic cell death pathway) by indirect inhibition of RIP1 kinase, with an EC50 value of 0.24 µM. |
| GSK872
GSK872 is a receptor interacting protein kinase-3 (RIP3) inhibitor, which inhibits kinase activity with an IC50 of 1.3 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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