t 614

Iguratimod (T614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.

DSS30 is a P25/CDK5 inhibitor.DSS30 acts by inhibiting the phosphorylation of amyloid precursor protein cleaving enzyme 1 (BACEl), which reduces the secretion of β-amyloid (Aβ).DSS30 can be used for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease.

α-NETA is a potent choline acetyltransferase (ChA) inhibitor and an ALDH1A1 and chemokine-like receptor 1 (CMKLR1) antagonist.Anti-cancer activity,Cholinesterase and acetylcholinesterase (AChE) inhibition,Dose-dependent reduction of body weight and fasting blood glucose levels in STZ-induced diabetic mice,Significantly reduced expression of renal injury markers,May be CEP-9722 can be used for the study of diabetic nephropathy.

APE1-IN-1 is a potent inhibitor of purine/pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells.

Nortadalafil (Demethyl Tadalafil) is demethyl Tadalafil, which is a PDE5 inhibitor, treating erectile dysfunction (ED) ; and under the name Adcirca for the treatment of pulmonary arterial hypertensio.

CXCR4 antagonist 6 (compound 46) is a highly potent small-molecule inhibitor of the chemokine receptor CXCR4 with an IC50 value of 79 nM, effectively suppressing CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, significantly inhibiting CXCL12/CXCR4-mediated cell migration, and demonstrating pronounced therapeutic efficacy in a mouse model of cancer metastasis, highlighting its value for cancer biology, metastasis research, and chemokine signaling studies.

SIRT5 inhibitor 4 (compound 11) is a dose-dependent and selective SIRT5 (Sirtuin5) inhibitor with an IC50 value of 26.4 μM for SIRT5 and no inhibitory effect on SIRT1/2/3 isoforms at 400 μM, with anticancer potential.

DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with anti-tumor activity, which also inhibits EGFR and HER2, and is useful for studying pancreatic cancer.

YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

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].

IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor that blocks IκBα phosphorylation in the NF-κB pathway.

FAK-IN-8 (compound 5h), a FAK inhibitor with an IC50 of 5.32 μM, exhibits potent anti-proliferative activity, making it suitable for use in cancer research [1].

InhA-IN-4 (TU14) is a potent inhibitor of Mycobacterium tuberculosis InhA (enoyl ACP reductase), with potential anticancer and antiproliferative activities for studying Mycobacterium tuberculosis infections.

Anticancer agent 47 (compound 4j) exhibits potent anticancer properties, demonstrating antiproliferative activities, inducing apoptosis, and causing cell cycle arrest at the G0/G1 phase. Moreover, Anticancer agent 47 has shown significant in vivo antitumor activities [1].