Mixed Lineage Kinase

亜型選択性的な製品

Mixed Lineage Kinase製品

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  • Mixed Lineage Kinase阻害剤 (6)
  • Mixed Lineage Kinase活性剤(1)
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S8251 Necrosulfonamide Necrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL).
Nature, 2024, 625(7995):585-592
Nat Commun, 2024, 15(1):7522
Cancer Lett, 2024, 585:216693
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
Sci Rep, 2024, 14(1):7739
J Exp Med, 2023, 220(9)e20230054
J Exp Med, 2023, 220(9)e20230054
S2805 LY364947 LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Rep Med, 2024, 5(2):101416
Cell Commun Signal, 2024, 22(1):242
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Cell Commun Signal, 2023, 21(1):82
Oncogene, 2023, 42(14):1132-1143.
Oncogenesis, 2023, 12(1):35
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
E1395 GW806742X GW806742X, is a potent inhibitor of MLKL (Mixed Lineage Kinase Domain-Like protein), and binds to the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X retards MLKL membrane translocation and inhibits necroptosis.
E2378 GNE-3511 GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of <0.5 nM.
S8251 Necrosulfonamide Necrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL).
Nature, 2024, 625(7995):585-592
Nat Commun, 2024, 15(1):7522
Cancer Lett, 2024, 585:216693
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
Sci Rep, 2024, 14(1):7739
J Exp Med, 2023, 220(9)e20230054
J Exp Med, 2023, 220(9)e20230054
S2805 LY364947 LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Rep Med, 2024, 5(2):101416
Cell Commun Signal, 2024, 22(1):242
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Cell Commun Signal, 2023, 21(1):82
Oncogene, 2023, 42(14):1132-1143.
Oncogenesis, 2023, 12(1):35
E1395 GW806742X GW806742X, is a potent inhibitor of MLKL (Mixed Lineage Kinase Domain-Like protein), and binds to the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X retards MLKL membrane translocation and inhibits necroptosis.
E2378 GNE-3511 GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of <0.5 nM.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182

Mixed Lineage Kinase阻害剤の選択性比較

Tags: MLK Inhibitors | MLKL Review