MAPK

RTIL 13 inhibits dynamin GTPase (IC50: 2.3 μM), targets its lipid binding domain, and suppresses endocytosis (IC50: 9.3 & 7.1 μM).

PROTAC SOS1 degrader-5 (compound 4) serves as an effective degrader of PROTAC SOS1, exhibiting a DC50 of 13 nM. It robustly suppresses the proliferation of NCI-H358 cells, with an IC50 value of 5 nM [1].

KP-14 is a PROTAC specifically designed to target KRAS.

GAGGVGKSAL, a wild-type KRAS G12D 10mer peptide, serves as an immunogenic neoantigen in cancer immunotherapy research [1].

<p>KRAS inhibitor-25 (compound 151a), a pyrido[2,3-d]pyrimidine derivative, effectively inhibits KRas G12V, KRas WT, and KRas G12R with IC50 values all below 100 nM.</p>

Peptide based on JIP-1(153-163) inhibits JNK with micromolar affinity; barely affects p38, ERK.

Mitogen-activated protein kinase 1 (MAPK1) activates the p38/NF-κB pathway and regulates cellular processes in sepsis-associated diseases.

KRAS G12D inhibitor 7, is a highly potent inhibitor specifically targeting KRAS G12D.

Deltasonamide 1 TFA: PDE6δ-KRas inhibitor, K D 203 pM, used in tumor research.

SCH772984 HCl selectively inhibits ERK1/2, acts like type I/II kinase inhibitors, and is potent at 4/1 nM IC50s in certain mutated tumor cells.

<p>Z16078526 promotes Ucp1, p38 MAPK, lipolysis, thermogenic genes, and mitochondrial activity in mouse brown adipocytes.</p>

Vacquinol-1 is an MKK4 activator, which rapidly and selectively induces glioma cell death.

(R)-5-hydroxy isoindolin-1-one is an RAS protein inhibitor with antiproliferative and antitumor properties.

HSND80 (Compound 1) is an orally active MNK/p70S6K inhibitor, exhibiting a Kd value of 44 nM for MNK1 and 4 nM for MNK2. The residence time of HSND80 on MNK1 and MNK2 is 45 minutes and 58 minutes, respectively. HSND80 effectively inhibits non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppresses the growth of triple-negative breast cancer (TNBC) cells in vitro.

KRas G12R inhibitor 1 targets mutant cysteines in K-Ras, binds irreversibly, and is used in cancer research.

Anti-osteoporosis agent-8 (Compound 4aa) is a RANKL inhibitor, capable of preventing RANKL-induced osteoclastogenesis and osteoclast differentiation, with an IC50 of 2.41 μM. Furthermore, Anti-osteoporosis agent-8 has been shown to mitigate bone loss in an ovariectomized (OVX) mouse model.

MLKL-IN-7 (compound 9) is an MLKL inhibitor that exhibits anti-necrotic activity in HT-29 cells, with an IC50 value of 148.4 nM.

<p>HPK1-IN-54 (Compound 16) is a potent inhibitor of HPK1 (hematopoietic progenitor kinase 1), enhancing T cell activation and proliferation by blocking HPK1 activity to exert antitumor effects. It has an IC50 of 2.67 nM for HPK1, showing excellent selectivity over the MAP4K family (&gt;100-fold) and other selected kinases (&gt;300-fold). HPK1-IN-54 exhibits moderate in vivo clearance and reasonable oral exposure in both mice and rats. Additionally, in the CT26 mouse colon cancer model, HPK1-IN-54 demonstrates significant antitumor activity and shows a synergistic effect when combined with anti-PD-1 therapy. HPK1-IN-54 holds promise for research in the field of immunology.</p>

VUBI1-octanoic acid is a conjugate of both the SOS1 ligand and linker, and it is applied in the synthesis of (4S)-PROTAC SOS1 degrader-1.

Cot inhibitor-1 hydrochloride blocks TPL-2 kinase (IC50=28nM) and TNF-α synthesis (IC50=5.7nM) in human blood.