T6265

Bosentan hydrate (Ro 47-0203) is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.

ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia capillaris and Rad3-related (ATR) kinases. As a promising lead compound for developing drugs targeting the ATR kinase, a key regulatory protein in the DNA damage response (DDR) that senses replication stress (RS), ATR-IN-11 has significant potential for cancer research.

CPL304110 is an orally active, selective and potent inhibitor of the fibroblast growth factor receptor FGFR (1-3), acting on FGFR1 (IC50: 0.75 nM), FGFR2 (IC50: 0.5 nM), FGFR3 (IC50: 3.05 nM).

FGFR-IN-2 (compound 1) is a potent FGFR inhibitor, targeting FGFR1 (IC50: 7.3 nM), FGFR2 (IC50: 4.3 nM), FGFR3 (IC50: 7.6 nM), and FGFR4 (IC50: 11 nM).

Fluocortin butyl ester is a developed corticosteroid compound with no detectable systemic corticosteroid activity when used topically. It appears to be an effective, well-tolerated topical steroid suitable for studies of perennial rhinitis.

BET bromodomain inhibitor 2 is a potent inhibitor of the BET-type bromodomain with an IC50 of 14.1 μM.

GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.

SHP504 is an inhibitor of SHP2 phosphatase and acts on SHP21-525 (IC50: 21 μM).

Antifungal agent 22 (compound D16) is an orally active antifungal agent with an IC50 of 0.5 μg/mL, exhibiting blood-brain barrier permeability, good metabolic stability, and low cytotoxicity. It selectively targets C. neoformans H99 cells by disrupting the integrity of the fungal cell membrane.

Cathepsin C-IN-4 is a potent inhibitor (IC50: 65.6 nM) of histone C. Cathepsin C-IN-4 inhibits THP-1 cells (IC50: 203.4 nM) and U937 cells (IC50: 177.6 nM).