MAPK Signaling

Darizmetinib is an inhibitor of mitogen-activated protein kinase kinase (MAP2K).

DS12881479 is an effective selective Mnk1 inhibitor with an IC50 value of 21 nM. It can be used for cancer research.

DS89002333 is an orally effective and potent inhibitor of PRKACA with an IC50 value of 0.3 nM. It exhibits good anti-tumor activity in a xenograft model derived from FL-HCC patients expressing the DNAJB1-PRKACA fusion gene. DS89002333 can be used for research on fibrolamellar hepatocellular carcinoma (FL-HCC).

Endothelin-1 (1-31) (Human) TFA is an effective vasoconstrictor and hypertensive agent. It is derived from the selective hydrolysis of big ET-1 by chymase.

GSK1790627 is the N-deacetylated metabolite of Trametinib. Trametinib is an orally active MEK inhibitor that activates autophagy and induces cell apoptosis.

KIF18A-IN-1 is an inhibitor of hematopoietic progenitor kinase 1 (HPK1), and more information can be found in compound I-47 in patent document WO2018102366A1.

ZYF0033 (HPK1-IN-22, compound ZYF0033) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of less than 10 nM based on its inhibitory effect on MBP protein phosphorylation. ZYF0033 reduces the phosphorylation of SLP76 (serine 376). ZYF0033 promotes anti-cancer immune response. ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased infiltration of DC, NK cells, and CD107a+CD8+ T cells into tumors but decreased infiltration of T cells, PD-1+CD8+ T cells, TIM-3+CD8+ T cells, and LAG3+CD8+ T cells.

HPK1-IN-32 is a highly selective, orally active small-molecule inhibitor of hematopoietic progenitor kinase 1 (HPK1/MAP4K1) with an IC 50 of 1.04nM.

JTP10-△-TATi TFA is a selective peptide inhibitor of JNK2, with an IC50 value of 92 nM. Its selectivity for JNK2 is more than 10 times that of JNK1 and JNK3.

NecroIr1 is an iridium (III) complex that induces necrosis in cisplatin-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 can activate receptor-interacting protein kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), regulating CDK4 expression.

NecroIr2 is an iridium (III) complex that induces necrosis in cisplatin-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 can activate receptor-interacting protein kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), regulating CDK4 expression.

OVA-E1 peptide TFA is an antagonist mutant of SIINFEKL [OVA (257-264)]. OVA-E1 peptide activates the p38 and JNK cascades in both mutant and wild-type thymocytes.

PKI (14-24)amide TFA is an effective inhibitor of PKA. In cell cytosol, PKI (14-24)amide strongly inhibits the activity of cyclic AMP-dependent protein kinase.

RLX-33 is an effective and selective relaxin family peptide 3 (RXFP3) antagonist with blood-brain barrier permeability. It also blocks the phosphorylation of ERK1/2 induced by relaxin 3, with IC50 values for RXFP3, ERK1, and ERK2 phosphorylation being 2.36 μM, 7.82 μM, and 13.86 μM respectively. RLX-33 can block the increase in food intake induced by the RXFP3 selective agonist R3/I5 in rats. RLX-33 can be used for research on metabolic syndrome.

TAK1-IN-4 (Compound 14) is a TAK1 inhibitor.

Trametiglue is a derivative of Trametinib that binds to KSR-MEK and RAF-MEK with unprecedented potency and selectivity through a unique interface interaction.

GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).

QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK.

MNK1/2-IN-5 is a potent and selective MNK1/2 inhibitor as a therapeutic agent.

HPK1-IN-26 is a HPK1 and GLK inhibitor extracted from patent WO2021254118A1 compound 1.

Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM).

Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK.

JNK-IN-11 (compound 1) is a potent JNK inhibitor with an IC50 value of 2.2, 21.4, 1.8 µM for JNK1, JNK2, JNK3, respectively.

DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM).