RIPK3
RIPK3 is a receptor-interacting serine/threonine kinase that drives necroptosis, a regulated inflammatory cell death pathway requiring RIPK3 and MLKL[1]. Mechanistically, RIPK3 phosphorylates MLKL, enabling MLKL oligomerization, plasma membrane localization, and necrotic membrane disruption[2][3]. In disease models, RIPK3-dependent necroptosis contributes to inflammatory injury, while RIPK3 also supports NLRP3 inflammasome activation through caspase-8 under IAP-deficient TLR signaling. Compared with RIPK1, RIPK3 shares RHIM-mediated necrosome signaling but lacks the same receptor-adaptor role; RIPK1 can both activate RIPK3 after receptor stimulation and suppress spontaneous RIPK3 activation in the cytosol[4]. For experimental applications, RIPK3 inhibitors such as GSK′840, GSK′843, and GSK′872 bind the RIPK3 kinase domain and inhibit enzyme activity, but these compounds can also induce RIPK3-dependent apoptosis[5]. - RIPK3 is central for studying necroptosis, MLKL phosphorylation, inflammatory signaling, and disease models. - RIPK3 inhibitors help dissect kinase-dependent signaling but require apoptosis controls in experimental design.
Verweise:
- [1]. Dhuriya YK, et al. Necroptosis: a regulated inflammatory mode of cell death. J Neuroinflammation. 2018 Jul 6;15(1):199. [Content Brief]
- [2]. Wang H, et al. Mixed lineage kinase domain-like protein MLKL causes necrotic membrane disruption upon phosphorylation by RIP3. Mol Cell. 2014 Apr 10;54(1):133-146. [Content Brief]
- [3]. Rodriguez DA, et al. Characterization of RIPK3-mediated phosphorylation of the activation loop of MLKL during necroptosis. Cell Death Differ. 2016 Jan;23(1):76-88. [Content Brief]
- [4]. Orozco S, et al. RIPK1 both positively and negatively regulates RIPK3 oligomerization and necroptosis. Cell Death Differ. 2014 Oct;21(10):1511-21. [Content Brief]
- [5]. Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95. [Content Brief]
-
RIPK3 Verwandte Produkte (26)
Verwandte Produkte (26)
-
Recombinant Proteins (3)
- 1
- 2
-
RIPK3-IN-8
0 ImagesArt. -Nr.: HY-189220RIPK3-IN-8 is an orally active and selective RIPK3 inhibitor with a Kd of 150 nM. RIPK3-IN-8 disrupts the formation of the RIPK3-MLKL necrosome and reduces the phosphorylation of downstream MLKL. RIPK3-IN-8 inhibits necroptosis. RIPK3-IN-8 increases the survival rate in a mouse model of TNF-α/Z-VAD-fmk (HY-16658B)-induced systemic inflammatory response syndrome. RIPK3-IN-8 is used for the research of systemic inflammatory response syndrome.
-
RIPK1-IN-42
0 ImagesArt. -Nr.: HY-184686RIPK1-IN-42 is an orally active RIPK1 inhibitor with a Kd of 21 nM. RIPK1-IN-42 inhibits the phosphorylation of RIPK1, suppresses the phosphorylation of downstream RIPK3 and MLKL, blocks necrosome formation, and inhibits necroptosis. RIPK1-IN-42 alleviates hypothermia, suppresses the elevation of pro-inflammatory cytokine levels, and reduces organ damage. RIPK1-IN-42 can be used for the research of systemic inflammatory response syndrome.
-
RIPK1-IN-39
0 ImagesArt. -Nr.: HY-180806CAS. Nr.: 3065634-42-3RIPK1-IN-39 (compound 2) is a potent and selective RIPK1 inhibitor (IC50 = 69.40 nM) exhibiting >100-fold selectivity over RIPK3 (IC50 = 6946 nM). RIPK1-IN-39 protects HT-22 and HT-29 cells from necroptosis by inhibiting the phosphorylation and activation of the RIPK1-RIPK3-MLKL pathway. RIPK1-IN-39 demonstrates neuroprotective effects in a rat model of middle cerebral artery occlusion (MCAO). RIPK1-IN-39 can be used for acute ischemic stroke (AIS) research.
-
WJH-C19
0 ImagesArt. -Nr.: HY-181596Reinheit: 98.65%WJH-C19 is an orally active RIPK1 inhibitor with an IC50 of 5.7 nM. WJH-C19 inhibits the RIPK1/RIPK3/MLKL signaling axis, blocks RIPK1 phosphorylation, suppresses the phosphorylation of downstream RIPK3 and MLKL, disrupts necrosome formation, and exhibits protective effects against necroptosis (Apoptosis) in multiple cell lines. WJH-C19 ameliorates symptoms of inflammatory bowel disease in a mouse colitis model by regulating the necroptosis pathway. WJH-C19 alleviates inflammation and bone destruction in a mouse model of rheumatoid arthritis. WJH-C19 is applicable to research related to inflammatory bowel disease and rheumatoid arthritis.
-
Ligustroflavone (Standard)
0 ImagesArt. -Nr.: HY-N0546RCAS. Nr.: 260413-62-5Synonyms: Nuezhenoside (Standard)Ligustroflavone (Standard) is the analytical standard of Ligustroflavone (HY-N0546). This product is intended for research and analytical applications. Ligustroflavone is an orally active flavonoid compound. Ligustroflavone can be extracted from Ligustrum lucidum. Ligustroflavone antagonizes the calcium-sensing receptor (CaSR), inhibits the RIPK1/RIPK3/MLKL pathway, and downregulates TGF-β/Smad signaling. Ligustroflavone regulates calcium metabolism, protects bone tissue, reduces cerebral ischemic injury, and inhibits liver fibrosis. Ligustroflavone can be used in the study of diabetic osteoporosis, ischemic stroke, and liver fibrosis.
- 1
- 2
