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Bleximenib (Menin-MLL inhibitor 24) (compound A) is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor. Bleximenib can be used for the research of cancer .
MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor targeting Mixed Lineage Kinase domain-like (MLKL). MLKL-IN-6 inhibits cell necrosis. MLKL-IN-6 inhibits MLKL phosphorylation and oligomerization during cell necrosis, inhibits immune cell death, and reduces the expression of adhesion factors. MLKL-IN-6 has low cytotoxicity, and it inhibits hepatic stellate cell activation, reduces liver fibrosis marker levels, and has anti-fibrotic effects .
URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction extracted from patent WO2017214367, compound example 1. Menin-MLL inhibitor 4 has antitumor activity .
MIV-6 is a small molecule inhibitor that inhibits menin-mixed lineage leukemia (MLL) interaction and exhibits strong selective activity in MLL leukemia cells with IC50 = 56 nM.
Enzomenib is an inhibitor of the menin protein encoded by the multiple endocrine neoplasia (MEN) gene. Enzomenib can block the binding of the menin protein to mixed lineage leukemia (MLL) fusion proteins and can be used in the study of hematological malignancies .
MIV-6R is an optimized small molecule inhibitor of menin-mixed lineage leukemia (MLL) interaction with IC50 = 56 nM, and its specific mechanism of action activity has been validated in MLL leukemia cells.
M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to treat MLL leukemia .
(S)-Bleximenib ((S)-Menin-MLL inhibitor 24) oxalate is a S-Enantiomer of (S)-Menin-MLL inhibitor 24 oxalate (HY-148669A). (S)-Bleximenib oxalate is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor, and can be used for the research of cancer .
MLK-IN-2 (Compound 9a) is a Mixed Lineage Kinase 3 (MLK3) inhibitor containing 3H-imidazole [4,5-b] pyridine structure. IC50 value is 6 nM. MLK-IN-2 can be used to study cancer and neurodegenerative diseases .
Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
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 .
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 .
Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide. Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
(E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
DDO-2213 is an orally active and potent WDR5-MLL1 inhibitor, with an IC50 of 29 nM and a Kd value of 72.9 nM for the WDR5 protein. DDO-2213 selectively inhibits MLL (mixed lineage leukemia) histone methyltransferase activity and the proliferation of MLL translocation-harboring cells. DDO-2213 can be used for MLL fusion leukemia research .
Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells .
MLKL-IN-3 (compound 66) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-3 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 31 nM . MLKL-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 82 nM . MLKL-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK4 expression .
MM-589 (racemic mixture) TFA, is a racemic mixture of MM-589 TFA (HY-100869A). MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome) .
NecroIr2 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), and regulates CDK4 expression .
RIPK3-IN-3 (compound 20) is a selective inhibitor of RIP kinase RIPK3 (IC50=10 nM). RIPK3 mediates the phosphorylation of Mixed Lineage Kinase (MLKL) and causes necroptosis, while RIPK3-IN-3 inhibits p-MLKL oligomerization and thereby inhibits necroptosis. RIPK3-IN-3 also downregulates CXCL5 secretion and inhibits AsPC-1 cell migration and invasion .
CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53 .
Anemarsaponin B is a steroidal saponin. Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
ML399 is a second-generation probe optimized for inhibitors of menin-mixed lineage leukemia (MLL) protein-protein interactions. Screening through the Molecular Library Probe Production Network (MLPCN) led to the discovery of several chemical classes, including piperidines, which successfully led to the generation of the first-generation probe ML227. However, metabolic instability, potency, and adjuvant pharmacological activity of ML227 were identified as limiting features. To enhance the utility of menin-MLL inhibitor probes for in vivo mechanistic studies, medicinal chemistry efforts were reinvigorated using a structure-based design approach, which ultimately led to the generation of the announced probe ML399. This study describes the structure-activity relationships and properties of this series of compounds.
Anemarsaponin B is a steroidal saponin. Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
MLKL protein is a pseudokinase that plays a key role in TNF-induced necroptosis. Despite lacking intrinsic kinase activity, it is activated through RIPK3 phosphorylation, leading to homotrimerization, plasma membrane localization, and execution of necroptosis. MLKL Protein, Human (His-SUMO) is the recombinant human-derived MLKL protein, expressed by E. coli , with N-6*His labeled tag. The total length of MLKL Protein, Human (His-SUMO) is 471 a.a., with molecular weight of ~59 kDa.
KMT2D Protein, a histone methyltransferase, methylates histone H3 'Lys-4' (H3K4), predominantly establishing H3K4me1 marks at active chromatin sites. Integral to chromatin remodeling, it functions as a coactivator for the estrogen receptor, recruited by ESR1, activating transcription. KMT2D's role in depositing specific histone marks at genomic locations underscores its crucial involvement in modulating chromatin structure and gene expression. KMT2D Protein, Human is the recombinant human-derived KMT2D protein, expressed by E. coli , with tag free. The total length of KMT2D Protein, Human is 155 a.a., .
KMT2D Protein, a histone methyltransferase, methylates histone H3 'Lys-4' (H3K4), predominantly establishing H3K4me1 marks at active chromatin sites. Integral to chromatin remodeling, it functions as a coactivator for the estrogen receptor, recruited by ESR1, activating transcription. KMT2D's role in depositing specific histone marks at genomic locations underscores its crucial involvement in modulating chromatin structure and gene expression. KMT2D Protein, Human (GST) is the recombinant human-derived KMT2D protein, expressed by E. coli , with N-GST labeled tag. The total length of KMT2D Protein, Human (GST) is 155 a.a., .
Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide. Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
MLK3 Antibody (YA3237) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3237), targeting MLK3, with a predicted molecular weight of 93 kDa (observed band size: 93 kDa). MLK3 Antibody (YA3237) can be used for WB, ICC/IF experiment in human background.
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