T6140

SB-334867 free base (SB334867A free base) is a selective orexin-1 (OX1) receptor antagonist. In CHO-OX1 cells, SB-334867 inhibits calcium responses mediated by the human OX1 receptor in a concentration-dependent manner, with a binding pKi value of 7.17 for the human OX1 receptor.

Anti-inflammatory agent 9 (compound 28) is a benzimidazothiazole derivative derived from tilomisole, exhibiting higher COX-2 enzyme affinity than COX-1, thereby demonstrating promising anti-inflammatory properties and oral bioavailability [1].

3-(3-Phenoxybenzyl)amino-β-carboline is a highly effective tubulin inhibitor, selectively degrading αβ-tubulin heterodimers, inducing cell cycle arrest and apoptosis in the G2/M phase, and displaying notable anticancer activity [1].

PGN36 (Compound 18) is a potent and highly selective antagonist of the cannabinoid CB2 receptor (CB2R), exhibiting exceptional affinity with a Ki value of 0.09 μM [1].

Plasma kallikrein-IN-3, a potent inhibitor ( IC 50 : 0.15 μM) of plasma kallikrein, finds application in research related to hereditary angioedema, diabetic macular edema, and diabetic retinopathy [1].

α-Synuclein inhibitor 3 (Compound 7g) is a potent inhibitor of α-synuclein (α-Syn) aggregation, with potential applications in Parkinson's disease research [1].

LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1].

RBM10-8 irreversibly inhibits human sphingosine-1- phosphate lyase (hS1PL) while behaving also as an enzyme substrate.

TRPC3/6-IN-1 is a highly potent and selective inhibitor that blocks the activity of canonical transient receptor channels TRPC3 and TRPC6, showing significant potency against human isoforms hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. This compound is valuable for research on chronic models of heart failure [1].

BChE-IN-2 (compound 22) is a highly effective inhibitor of BChE, with a Ki value of 0.099 μM, and represents a promising pyrimidine and pyridine derivative for investigating Alzheimer's disease (AD). [1]

CXCR4 antagonist 3 (compound 12a), an effective antagonist of CXCR4, exhibits an IC50 of 11 nM. It is a congener of TIQ15, showcasing exceptional properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. With its potential for research on the human immunodeficiency virus, CXCR4 antagonist 3 holds great promise [1].