| S8251 |
Necrosulfonamide
|
Necrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL).
|
-
Nature, 2025, 10.1038/s41586-025-09741-1
-
Nature, 2025, 647(8090):735-746
-
Cell Metab, 2025, S1550-4131(25)00149-4
|
|
| 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. This compound also inhibits ABL1 with IC50 of 6.8 nM. It 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. This compound retards MLKL membrane translocation and inhibits necroptosis.
|
-
Commun Biol, 2025, 8(1):573
-
BMC Oral Health, 2025, 25(1):941
|
|
| E2378 |
GNE-3511
|
GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of <0.5 nM.
|
|
|
| S8032 |
PRT062607 (P505-15) HCl
|
PRT062607 (P505-15, BIIB057, PRT-2607) HCl 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 Adv, 2025, 11(31):eadu4270
-
Sci Rep, 2024, 14(1):7739
-
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
|
|
| 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. This compound exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. It induces apoptosis and caspase-3 and caspase-8 activity. This chemical increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
|
-
bioRxiv, 2025, 2025.07.17.665404
-
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
-
Phytomedicine, 2022, 102:154182
|
|