h-358

KRAS inhibitor-9 (DUN09716) is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSC-LC cells with KRAS mutation but not normal lung cells

MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK/PD experiment.

NVP-231 is a potent, specific and reversible CerK inhibitor(IC50=12±2 nM) that competitively inhibits ceramide binding to CerK.

CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSC-LC cells, with analgesic, anti-inflammatory and anti-cancer activities.

Amicarbazone (BAY-MKH3586; BAY314666) is a potent PSII inhibitor, disrupting photosynthetic electron transport by binding to the Qb domain of photosystem II. This broad-spectrum herbicide is effective through foliar and root application, showcasing rapid absorption and translocation. However, its effectiveness can be compromised by common PSII inhibitor resistance. With an IC50 value indicating high potency, amicarbazone leads to chlorosis, stunted growth, tissue necrosis, and death in sensitive plants. Despite these severe effects, it exhibits good selectivity and outperforms atrazine as a herbicide, allowing for its application at lower doses compared to traditional photosynthetic inhibitors.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

RBC8 is a specific GTPases RalA/RalB inhibitor by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases RhoA and Ras.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

BAY 1892005 is a p53 protein modulator that targets the p53 condenser for the study of diseases associated with misfolded p53 protein