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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
22 Results for "
necroptotic
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "necroptotic" in MCE Product Catalog:
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25 Publications Verification
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GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X has activity against VEGFR2 (IC50=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis .
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25 Publications Verification
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GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis .
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ALDH1A inhibitor 673A is an ALDH1A inhibitor with IC50s of 246 nM (ALDH1A1), 230 nM (ALDH1A2), 348 nM (ALDH1A3), respectively. ALDH1A inhibitor 673A has little or no inhibitory effect on other ALDH family members. ALDH1A inhibitor 673A induces necroptotic ovarian cancer stem-like cells (CSCs) death. ALDH1A inhibitor 673A induces DNA double stand breaks in cancer cells. ALDH1A inhibitor 673A can be used for the study of ovarian cancer .
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Quinones other families Phenols Polyphenols Plants Disease Research Fields Naphthalene Quinones Cancer
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1 Cited Publications
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PROTAC MLKL Degrader-1 is a selective MLKL PROTAC degrader with a DC50 of 2.4 μM. PROTAC MLKL Degrader-1 blocks necroptosis without modulating the phosphorylation of RIPK1 or RIPK3, and exhibits a linear correlation between MLKL levels and necroptotic cell death .
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AV123 (compound 12) is a non-cytotoxic RIPK1 inhibitor (IC50=12.12 µM). AV123 blocks the TNF-α-induced necroptotic (EC50=1.7 μM) but not the apoptotic cell death. AV123 can be used in the study of necrotic chronic conditions such as ischemia-reperfusion injury of the brain, heart and kidney, inflammatory diseases, neurodegenerative diseases and infectious diseases .
Cat. No.: HY-177119
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ZBP1 Covalent PROTAC-1 is a covalent PROTAC degrader targeting ZBP1, with a DC50 of 25.69 nM. ZBP1 Covalent PROTAC-1 integrates a ZBP1-binding DNA aptamer, a linker containing covalent NASA, and an E3 ligase-recruiting moiety to guide ubiquitin-proteasome system-mediated degradation of ZBP1. ZBP1 Covalent PROTAC-1 exhibits inhibitory activity against necroptosis signaling pathways and inflammatory responses. ZBP1 Covalent PROTAC-1 can be used for research on viral pneumonia .
Cat. No.: HY-162424
CAS No.: 3057611-79-4
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ZBP1/RIP3/MLKL activator 1 (compound 3a) is a synthetically derived quinoline compound. ZBP1/RIP3/MLKL Activator 1 induces DNA damage, enhances intracellular levels of reactive oxygen species (ROS), and triggers apoptosis via the caspase pathway. Furthermore, when apoptosis is inhibited, ZBP1/RIP3/MLKL Activator 1 promotes necroptotic cell death through the ZBP1-RIP3-MLKL pathway. ZBP1/RIP3/MLKL Activator 1 is utilized in oncological research, particularly in the selective targeting of cells with impaired apoptotic function .
Cat. No.: HY-24504
CAS No.: 305866-70-0
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MBA-m1 is a reversible non-covalent allosteric inhibitor of mMLKL2, with a Kd value of 6 μM for mMLKL2. MBA-m1 delays Necroptosis. MBA-m1 has no effect on the activities of RIPK1 or RIPK3. MBA-m1 alleviates skin injury, epidermal thickening and immune cell infiltration in dermatitis models, and reduces aortic diameter enlargement and structural changes in abdominal aortic aneurysm models. MBA-m1 can be used in research related to dermatitis and abdominal aortic aneurysm .
Cat. No.: HY-P990258
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Cat. No.: HY-148767
CAS No.: 2755872-58-1
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MLKL-IN-5 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with a KD of < 10 nM. MLKL-IN-5 exhibits selectivity for RIP3 and RIP1, with KD values of 1-30 μM and > 30 μM, respectively. MLKL-IN-5 mediates necroptosis .
Cat. No.: HY-178163
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Zharp1-163 is a dual inhibitor of ferroptosis and necroptosis. Zharp1-163 effectively blocks ferroptosis by reducing reactive oxygen species (ROS) levels and inhibits necroptosis by potently and selectively targeting RIPK1 kinase activity (KD = 240 nM; IC50 = 406.1 nM). Zharp1-163 inhibits the cellular activation of RIPK1, RIPK3 and MLKL in response to necroptotic stimulation. Zharp1-163 markedly attenuates TNF-α (HY-P1875)-induced systemic inflammatory syndrome, including the prevention of TNF-α-induced mortality and hypothermia in mice. Zharp1-163 significantly alleviates acute kidney injury associated with both necroptosis and ferroptosis in models induced by Cisplatin (HY-17394) and ischemia-reperfusion. Zharp1-163 can be used for the study of diseases associated with cell death pathways, such as kidney disease .
Cat. No.: HY-146758
CAS No.: 2919964-79-5
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RIPK1-IN-14 (Compound 41) is a potent inhibitor of RIPK1 with an IC50 value of 92 nM. RIPK1-IN-14 shows a significant anti-necroptotic effect in a necroptosis model in U937 cells .
Cat. No.: HY-169072
CAS No.: 3103327-20-1
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PROTAC MLKL Degrader-2 is an orally active and highly selective mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC degrader with a DC50 of 0.012 μM. PROTAC MLKL Degrader-2 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, leading to ubiquitination of MLKL and its degradation via a proteasome-dependent pathway. PROTAC MLKL Degrader-2 inhibits necroptosis, reduces ROS production, restores mitochondrial function, and ameliorates lysosomal dysfunction induced by necroptotic stimuli. PROTAC MLKL Degrader-2 degrades MLKL in xenograft mouse models. PROTAC MLKL Degrader-2 can be used in cancer-related research .
Cat. No.: HY-157963
CAS No.: 3031534-16-1
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RIPK1-IN-23 (compound 19) is a RIPK1 inhibitor with potent anti-necroptotic effects in HT-29 cells (EC50 of 1.7 nM). RIPK1-IN-23 shows anti-inflammatory activities .
Cat. No.: HY-149052
CAS No.: 2919801-86-6
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SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a Kd of 85 nM. SZM-1209 exhibits high anti-necroptotic activity (EC50=22.4 ± 8.1 nM). SZM-1209 shows anti-SIRS (systemic inflammatory response syndrome), and anti-ALI (acute lung injury) effects .
Cat. No.: HY-170232
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RIPK1-IN-29 (Compound 22) is a RIPK1 inhibitor, with an IC50 of 6.9 nM. RIPK1-IN-29 exerts anti-necroptotic (Apoptosis) activity by inhibiting RIPK1. In a TNF-α-induced in vivo inflammation model, at a dose of 10 mg/kg, RIPK1-IN-29 can protect mice from hypothermia and death. RIPK1-IN-29 can be applied to the research field of inflammatory diseases .
Cat. No.: HY-181944
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RIPK1-IN-40 (Compound 51) is a RIPK1 inhibitor and anti-necroptotic agent (with an EC50 of 0.07 μM against necroptosis). RIPK1-IN-40 binds to the kinase domain of RIPK1, forms hydrogen bond interactions with Met95, and establishes additional polar contacts with Asp156 to stabilize binding, thereby inhibiting necroptosis. RIPK1-IN-40 can be used for the research of colorectal cancer .
Cat. No.: HY-179680
CAS No.: 3092834-30-2
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RIPK1-IN-38 is an orally active RIPK1 inhibitor with an IC50 value of 27 nM. RIPK1-IN-38 can inhibit the phosphorylation of RIPK1 and its downstream signaling molecules RIPK3 and MLKL. RIPK1-IN-38 exhibits anti-necroptotic activity. RIPK1-IN-38 has excellent anti-inflammatory efficacy in both the SIRS model and GVHD model. RIPK1-IN-38 can be used for the research of inflammatory and immune-related diseases .
Cat. No.: HY-184001
CAS No.: 3078683-57-2
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LT-1339-553 is a selective, orally active RIPK1 inhibitor with IC50 values of 4.32, 95.74 and 84.33 nM against RIPK1, RIPK2 and RIPK3, respectively. LT-1339-553 exerts anti-necroptotic activity by inhibiting the AKT/PI3K/NF-κB pathway and the IL-17 pathway. LT-1339-553 reduces liver injury, inflammatory responses and collagen deposition. LT-1339-553 can be used in studies related to schistosomiasis-induced liver fibrosis .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
