NCDM-32B is a novel potent and selective KDM4 inhibitor, impairing viability and transforming phenotypes of basal breast cancer.

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.

Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive

VX-984 (M 9831) is a potent, selective inhibitor of DNA-PK with IC50 of 88±64 nM for inhibition of DNA-PKcs autophosphorylation (Ser2056) in A549 lung cancer cells, with good selectivity versus other PI3K family members..

γ-AA peptide P6 (Cyclic γ-AA P6) is a potent activator of E6 associated protein (E6AP). γ-AA peptide P6 can stimulate the self-ubiquitination of E6AP and E6AP-catalyzed substrate ubiquitination in reconstituted reactions in vitro. γ-AA peptide P6 can also enhance the ubiquitination of E6AP substrates in the cell and accelerate their degradation by the proteasome.

MCC7840 sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. MCC7840 sodium can be used for the research of inflammatory diseases.

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.

cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.

Novel RBP4 antagonist with good in vitro potency and selectivity and optimal rodent pharmacokinetic (PK) and pharmacodynamic (PD) characteristics

IK930 (compound I-32) is a potent and orally active TEAD inhibitor with an EC50 value of <0.1 µM.

TT-10 is a novel multifaceted fluorinated compound with promising features of CM proliferative, antioxidant, and antiapoptotic activities in vitro.

CI-976 (PD 128042) is a potent, selective, orally bioavailable inhibitor of ACAT-1 (Acetyl-CoA acetyltransferase 1) with IC50 of 73 nM.

PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.

A sphingosine 1-phosphate (S1PR) receptor agonist

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.

Shield-1 is a cell-permeable FKBP ligand that is designed to protect an otherwise unstable protein domain from degradation; binds tightly to FKBP, induces rapid and processive degradation of the LID domain.

Nrf2-Activator is a potent Nrf-2 activator.

Flupenthixol dihydrochloride is a typical antipsychotic of the thioxanthene class that acts as an antagonist at dopamine D2 receptors (Ki = 0.38 nM) and an inverse agonist at serotonin 5-HT2A receptors (Ki = 7 nM).1 It has also been identified as an inhib

Selective RIP3 kinase inhibitor

(E/Z)HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.

Selnoflast (example 6) is a NLRP3 inhibitor (extracted from patent WO2019008025).

QcrB inhibitor TB47 (TB47) is a novel antimycobacterial agent that fuctions as a putative respiratory complex III (QcrB) inhibitor with MIC of 0.016-0.5 ug/mL against a panel of 56 M. tuberculosis clinical isolates.

BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM. show good metabolic stability in vitro and high oral bioavailability in vivo.

TACH101 (QC8222, TACH 101) is a reversible, α-ketoglutarate competitive, selective and potent inhibitor of KDM4 isoforms A-D with IC50 values of <0.1 uM against all four isoforms.TACH101 demonstrated potent increase of H3K36me3 levels (EC50 <0.001 uM, HTRF) in KYSE-150 cell line engineered to overexpress KDM4C and showed potent anti-proliferative activity in multiple cell lines in OncoPanel.Sub-micromolar levels of TACH101 induced apoptosis in human colorectal (HT-29), esophageal (KYSE-150), and triple negative breast cancer (MDA-MB-231) cell lines with EC50s of 0.033-0.092 uM.TACH101 triggered effective tumor growth control in xenograft models including colorectal, esophageal, gastric, breast, and lymphoma with tumor growth inhibition of up to 100%.

SBP-3264 is a valuable chemical probe for understanding the roles of STK3 and STK4 in acute myeloid leukemia (AML).

Dihydroresveratrol is an SIRT1 activator. It is a primary metabolite of resveratrol.

10-Hydroxycanthin-6-one is an antileukemic canthin-6-one alkaloid from Brucea antidysenterica. Antitumor agent.

9-Hydroxycanthin-6-one is an alkaloid compound. 9,10-Dimethoxycanthin-6-one exhibits NF-κB inhibitory effects with an IC50 of 3.8 μM.

9-Methoxycanthin-6-one, a canthin-6-one alkaloid, is present in intact plant parts and in callus tissues of different explants. 9-Methoxycanthin-6-one shows anti-tumor activity.

Canthin-6-one displays a wide range of biological activities, such as antimycobacterial activity.