T6240

Palbociclib Isethionate (PD 0332991 isethionate) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Anti-infective agent 4 (compound 73) is an orally active Trypanosoma cruzi inhibitor with an IC50 of 0.016 μM. It effectively reduces parasite burden in vivo and is useful for studying infections.

TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-type calcium channels. It effectively penetrates the CNS and blocks natural T-type currents in deep cerebellar nucleus neurons, completely eliminating window currents in wild-type and mutant Cav3.1 channels. [research]

DM-01 is a potent and selective inhibitor of EZH2. DM-01 can be used to study diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL) and SNF5/INI-1/SMARCB1 gene-associated solid tumours.

SHMT-IN-2 (compound 2) is a specific human SHMT1/2 small molecule inhibitor that acts on SHMT1 (IC50: 13 nM) and SHMT2 (IC50: 66 nM). SHMT-IN-2 inhibits the growth of many human cancer cells and is sensitive to B-cell lymphoma.

KDM1/CDK1-IN-1 (compound 4) is a potent inhibitor of KDM1 (IC50: 0.096 μM) and CDK1 (IC50: 0.078 μM), blocking the cell cycle of HOP-92 cells in the G2/M phase and inducing apoptosis. It is highly cytotoxic to CCRF-CEM cells (IC50: 16.34 μM), HOP-92 cells (IC50: 3.45 μM), and Hep-G2 cells (IC50: 7.79 μM).

Nur77 modulator 2 is a Nur77 regulator with a Kd value of 0.35 μM. Nur77 modulator 2 is also a potent, orally active inhibitor of inflammation. nur77 modulator 2 regulates Nur77 co-localization in mitochondria.

PDHK-IN-4 (Compound 30) is a potent inhibitor of PDHK, targeting PDHK2 (IC50: 0.0051 μM) and PDHK4 (IC50: 0.0122 μM), with potential applications in cancer research.

PI3Kδ-IN-11 is a potent and selective PI3Kδ inhibitor (IC50: 27.5 nM) that dose-dependently blocks PI3K/Akt pathway activity. PI3Kδ-IN-11 can be used in B- or T-cell-associated malignancy studies.