T6437

Cefoperazone (Medocef) binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. It can inhibit rMrp2-mediated [3H]E217βG uptake (IC50: 199 μM).

JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia.

QN523 represents a novel scaffold with drug-like properties, showing potent in vitro cytotoxicity in a panel of 12 cancer cell lines. QN523 shows significant in vivo efficacy in a pancreatic cancer xenograft model. Autophagy is a major mechanism of action.

Casein kinase 1δ-IN-9 is a Quinone reductase 2 inhibitor with IC50 of 0.6μM.

Virodhamine (O-arachidonoyl ethanolamine), an endocannabinoid, is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine can be used for the research of neurological disorders such as Alzheimer's diseases.

CDK1-IN-2 (cdk1 inhibitor 2) is a CDK1 inhibitor with IC50 of 5.8 μM. A broad-spectrum kinase profiling of CDK1-IN-2 revealed nonselective inhibition of several kinases.

UNC 1021 is a selective L3MBTL3 inhibitor (IC50 = 0.048 μM).

AZD0095 is a selective inhibitor of MCT4 with an IC50 of 1.3 nM.