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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
19 Results for "
nek7 inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "nek7 inhibitor" in MCE Product Catalog:
12
12 Publications Verification
Cat. No.: HY-N0373
CAS No.: 58749-23-8
3
3 Cited Publications
ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9 .
1
1 Cited Publications
Cat. No.: HY-N3005
CAS No.: 33627-28-0
1
1 Cited Publications
Cat. No.: HY-163358
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
SLC3037 is a NLRP3 inhibitor which blocks NLRP3 from binding to NEK7 or oligomerization, inhibiting inflammasome caused by MSU and other inflammasome activators. SLC3037 can be used for research of gout, cardiovascular diseases, metabolic syndrome or neurodegenerative diseases .
Cat. No.: HY-159520
CAS No.: 2731294-23-6
Synonyms: Ofirnoflast; HT-6184
Research Areas:
Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia .
Cat. No.: HY-172162
Target:
Research Areas:
LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia .
Cat. No.: HY-176860
CAS No.: 3069891-91-1
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
NEK7 degrader-1 is a NEK7 molecular glue degrader with a DC50 of 9 nM. NEK7 degrader-1 dose-dependently inhibits caspase-1 activity and IL-Ιβ release in macrophages in response to NLRP3 inflammasome activation. NEK7 degrader-1 can be used for autoinflammatory and autoimmune disorders like multiple sclerosis, neurodegeneraive diseases like Alzheimer's disease and cardiovascular and melabolic disorders like pericarditis and Type 2 diabetes research .
Cat. No.: HY-173154B
Research Areas:
NK7-902 diTFA is a selective and orally active CRBN-dependent NEK7 molecular glue degrader with Kd values of 1.5 and 2.6 μM for hNEK7 and mNEK7. NK7-902 diTFA fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 diTFA shows activity in murine systems and induces a profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation. NK7-902 diTFA can be used for the research of inflammation, such as cryopyrin-associated periodic syndromes .
Cat. No.: HY-174270
CAS No.: 3088796-72-6
Research Areas:
NLRP3-IN-79 is an orally active NLRP3 inhibitor. NLRP3-IN-79 inhibits NLRP3 inflammasome with an IC50 of 10.69 nM. NLRP3-IN-79 blocks NLRP3 inflammasome assembly by directly binding to NLRP3 and disrupting the NEK7-NLRP3 interaction. NLRP3-IN-79 can be used for the study of NLRP3-driven diseases model, including systemic inflammation, peritonitis, and colitis .
Cat. No.: HY-168737
Research Areas:
NEK7-IN-2 is a NEK7 inhibitor. NEK7-IN-2 increases the thermal stability of NEK7, disrupts the NEK7-NLRP3 interaction, inhibits NLRP3 inflammasome assembly, and suppresses the release of IL-1β (with an IC50 of 0.048 μM against IL-1β). NEK7-IN-2 can be used for the research of inflammatory diseases .
Cat. No.: HY-169933
CAS No.: 2738569-12-3
Target:
Research Areas:
NEK7-IN-1 (Compound I-15) is the inhibitor for NIMA-related kinase 7 NEK7 with IC50 <100 nM. NEK7-IN-1 inhibits the IL-1β release with IC50 <50 nM .
Cat. No.: HY-163756
CAS No.: 2769903-01-5
Target:
Research Areas:
NLRP3-IN-43 (compound II-8) is a poteny inhibitor of NLRP3 inflammasome activation that binds to the LRR domain, and disrupts NLRP3-NEK7 interaction .
Cat. No.: HY-208735
CAS No.: 3120512-57-1
Target:
Research Areas:
NEK7 degrader-5 is a NEK7 degrader. NEK7 degrader-5 inhibits the release of proinflammatory cytokines IL-1β and IL-18. NEK7 degrader-5 can be used for the research of inflammatory and tumor diseases .
Cat. No.: HY-N0373R
CAS No.: 58749-23-8
Cat. No.: HY-185311
CAS No.: 3119435-52-5
Research Areas:
NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation .
Cat. No.: HY-180890
Target:
Research Areas:
PPARγ agonist-21 (Compound 9a) is a PPARγ agonist with an EC50 of 3.12 μM. PPARγ agonist-21 activates PPAR-γ to inhibit NF-κB and attenuate NLRP3 inflammasome assembly. PPARγ agonist-21 blocks NLRP3-ASC and NLRP3-NEK7 interaction. PPARγ agonist-21 attenuates the severity of gouty arthritis .
Cat. No.: HY-181488
CAS No.: 3097745-69-9
Research Areas:
NLRP3-IN-87 is a selective and orally active NLRP3 inhibitor with a Kd of 0.23 μM. NLRP3-IN-87 binds directly to the NLRP3 NACHT domain, disrupts NLRP3-NEK7 and NLRP3-ASC interactions, inhibits ASC oligomerization, and blocks inflammasome assembly. NLRP3-IN-87 suppresses caspase-1 activation and IL-1β secretion. NLRP3-IN-87 exhibits anti-inflammatory and analgesic activity, reducing joint swelling, inflammation, and pain in an MSU (HY-B2130A)-induced acute gout mouse model. NLRP3-IN-87 can be used for the research of gout .
Cat. No.: HY-182380
CAS No.: 1632152-27-2
Target:
Research Areas:
ODZ10117 is a STAT3 and NLRP3 inhibitor with a human STAT3 SH2 domain IC50 of 7.5 μM. ODZ10117 binds to the STAT3 SH2 domain, suppressing tyrosine phosphorylation, dimerization, nuclear translocation, and transcriptional activity. ODZ10117 binds to NLRP3, impairs NEK7 interaction, prevents inflammasome formation, and inhibits caspase-1 and IL-1β cleavage.ODZ10117 reduces MSU (HY-B2130A)-induced IL-1β release, lowers LPS (HY-D1056)-induced sepsis mortality, and exhibits anti-inflammatory effects. ODZ10117 induces apoptosis, suppresses breast cancer cell migration and invasion, reduces tumor growth and lung metastasis, and extends survival in breast cancer models. ODZ10117 can be used for the research of Monosodium urate (HY-B2130A)-induced peritonitis, LPS-induced sepsis, breast cancer, glioblastoma, and Alzheimer's disease .
Cat. No.: HY-179635
CAS No.: 3114128-67-2
Research Areas:
GSTO1-IN-6 is an allosteric and covalent GSTO1 inhibitor with an IC50 of 457 nM. GSTO1-IN-6 markedly reduces Lipopolysaccharides (LPS) (HY-D1056)-induced IL-1β (IC50 of 1.9 μM) and IL-18 (IC50 of 10. μM) secretion in human monocyte-derived macrophages. GSTO1-IN-6 covalently modifies GSTO1-Cys32, inducing conformational changes and protein destabilization. GSTO1-IN-6 can be used for the research of inflammatory diseases .
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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
