T6408

Betaxolol (Kerlone) is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.

Clazosentan (Ro 61-1790) is a selective antagonist of the endothelin A receptor (ETAreceptor) that inhibits ET-1-mediated vasoconstriction, preventing cerebral vasospasm and vasospasm-associated cerebral infarction.

c-Met-IN-12 is a selective, orally active type II c-Met kinase inhibitor (IC50: 10.6 nM). c-Met-IN-12 is a high inhibitor of AXL, Mer and TYRO3 kinases (>80% inhibition at 1 μM). c-Met-IN-12 can be used as a scaffold to further enhance kinase selectivity. c-Met-IN-12 exhibits anti-tumour activity.

BPN-15606 besylate is a potent, orally active γ-secretase regulator (GSM) that reduces the production of Aβ42 (IC50: 7 nM) and Aβ40 (IC50: 17 nM) by SHSY5Y neuroblastoma cells. BPN-15606 besylate exhibited good PK/PD properties (including bioavailability, half-life and clearance).

ABC44 is a potent inhibitor of serine hydrolase with IC50s of 0.1 μM and 6.5 μM for palmitoyl protein thioesterase 1 (PPT1) in situ and in vitro, respectively. ABC44 can be used to study late infantile neuron-like lipofuscinosis.

MMP-9-IN-5 is an MMP-9 inhibitor with an IC50 value of 4.49 nM and is able to form hydrogen bonds with MMP-9. MMP-9-IN-5 also inhibits AKT activity with an IC50 value of 1.34 nM. MMP-9-IN-5 exhibits cytotoxicity, induces apoptosis and can be used in cancer research.

KRAS G12C inhibitor 43 is a potent inhibitor of KRAS G12C and inhibits the migration and proliferation of H358 cells (IC50: 0.001-1 μM μM), A549 cells (IC50>1 μM) and HCC cells (IC50>1 μM).

PD-1/PD-L1-IN-20 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interaction, blocking the interaction with an IC50 of 5.29 nM. PD-1/PD-L1-IN-20 can be used to study cancer, infectious diseases, and autoimmune diseases.

GZD856 formic is a potent, orally active inhibitor of PDGFRα/β and Bcr-Abl T315I, demonstrating IC50 values of 68.6 nM and 136.6 nM for PDGFRα/β, respectively, and 19.9 nM and 15.4 nM for native Bcr-Abl and the T315I mutant, respectively. This compound exhibits significant antitumor activity.

Lafadofensine D-(-)-Mandelic acid is a monoamines reuptake inhibitor with sufficient efficacy for short-term administration.

BRD4 D1-IN-1 is a selective inhibitor of BRD4 D1 with an IC50 <0.092 μM, an affinity of 18 nM, and over 500-fold selectivity for BRD4 D1 and BRD4 D2.