r 14

Amchem R 14 is a biochemical.

GSK-3β inhibitor 14 (1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-2-methyl-5-(phenylmethyl)-) is a weak GSK-3β inhibitor, IC50﹥ 100μM.

Fluprostenol isopropyl ester, a potent agonist of the F-series prostaglandin receptor, serves as a prodrug utilized clinically as an ocular hypotensive agent for glaucoma treatment. An impurity, 13(R),14(R)-epoxy fluprostenol isopropyl ester, arises during its production, existing as a chiral enantiomer of the epoxide. The pharmacological properties of this specific enantiomer have yet to be thoroughly investigated.

14:0 Hemi BMP (S,R) ammonium is a bis(monoacylglycerol) phosphate (BMP) compound.

KRAS G12C inhibitor 14 is a potent compound with an IC50 of 18 nM [1].

SR 146131 is a potent and selective agonist of the nonpeptide receptor.

WRN inhibitor 14 (compound S35) is an orally administered WRN inhibitor with anticancer properties. It effectively suppresses tumor growth in the SW48 xenograft model in BALB/c nude mice.

p53 Activator 14 (Compound 7A) is a derivative of Neratinib that can induce DNA damage and activate p53, thereby inhibiting the proliferation of various cancer cells, with an IC50 of 7.21 μM for HCT116 cells. This compound hinders adhesion, migration, and invasion of HCT116 cells, disrupts the cell cycle, and triggers apoptosis. In addition, p53 Activator 14 exhibits anti-tumor properties and inhibits angiogenesis in the chick embryo chorioallantoic membrane (CAM) model.

SR 142948-C3-NHMe is the methylated form of SR 142948.

Protein kinase inhibitor 14 (Compound 13) exhibits inhibitory effects on various serine/threonine kinases and receptor/non-receptor tyrosine kinases.

Topoisomerase I inhibitor 14 (Compound 4h) acts as an inhibitor of topoisomerase I. It suppresses the proliferation of A549 and C6 cells, with IC50 values of 4.56 μM and 13.17 μM, respectively. The compound shows no significant toxicity towards healthy NIH3T3 cells (IC50 of 74.44 μM) and demonstrates anticancer activity.

Apoptosisinducer 14 (Compd 7f) is a reagent utilized in chemotherapy research, capable of inducing p53-mediated apoptosis. The IC50 values of Apoptosisinducer 14 are 193.93 μg/mL in A549 cells, 6.76 μg/mL in HCT116 cells, and 222.67 μg/mL in HF84 cells.

SR 142948 TFA is an orally active, selective non-peptide neurotensin receptor (NT) antagonist, displaying IC50 values of 1.19 nM in h-NTR1-CHO cells, 0.32 nM in HT-29 cells, and 3.96 nM in adult rat brain. In HT-29 cells, it counteracts NT-induced inositol monophosphate formation with an IC50 of 3.9 nM. It blocks NT-induced hypothermia, analgesia, and turning behavior in vivo and can cross the blood-brain barrier, making it useful for research in psychiatric disorders.

PROTACEGFRdegrader 14 is a potent and selective EGFR PROTAC degrader with a DC50 value of approximately 2.9 nM against EGFRL858R/T790M/C797S and a Dmax of 93.1%. It induces the selective degradation of EGFRC797S via a VHL and proteasome-dependent mechanism, downregulating EGFR-related transcriptomes. PROTACEGFRdegrader 14 exhibits high selectivity for EGFRWT, induces cell cycle arrest and apoptosis, and effectively inhibits tumor growth. It is applicable for research on non-small cell lung cancer (NSCLC).

platelet fibrinogen receptor glycoprotein IIb/IIIa (GpIIb/IIIa) antagonist

5-HT6 antagonist,selective and high affinity

SR 140333 is a NK1 receptor antagonist.

SR 142948 is a neurotensin (NT) receptor antagonist.

NK3 receptor antagonist

Tubulin inhibitor 14 is a potent inhibitor of NQO2 (quinone oxidoreductase 2) with an IC50 of 1.0 μM, which also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. As a microtubule destabilizer, Tubulin inhibitor 14 has potential tumor-selective, anti-angiogenic, and vascular-destructive properties [1].

Carbonic anhydrase inhibitor 14 (Compound 8b) is a potent CA inhibitor, exhibiting K i values of 1203, 99.7, 9.4, and 27.7 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. Additionally, it effectively inhibits CDK2 with an IC 50 of 20.3 μM and demonstrates significant antitumor activity [1].

KRAS G12D inhibitor 14 is a potent compound that binds the KRAS G12D protein (Kd: 33 nM) and selectively inhibits the active form KRAS G12D-GTP, but not KRAS G13D.

ATX inhibitor 14, an indole-based carbamate derivative, is a potent inhibitor (IC50: 0.41 nM) of self-adhesive proteins (ATX) and has shown potential for research in fibrosis-related diseases.

SR 142948 dihydrochloride is a selective, orally active, non-peptide neurotensin receptor (NT) antagonist, featuring IC50 values of 1.19 nM, 0.32 nM, and 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. It effectively inhibits NT-induced inositol monophosphate formation in HT-29 cells (IC50 = 3.9 nM) and blocks NT-induced hypothermia, analgesia, and steering behavior in vivo. Furthermore, it demonstrates blood-brain barrier permeability, positioning it as a potential tool for psychiatric disorder research [1] [2].