Showing 849–864 of 5741 results

Olmutinib (HM61713, BI 1482694)

Olmutinib is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton’s tyrosine kinase.

Selonsertib (GS-4997)

GS-4997 is a highly selective and potent once-daily oral ASK1 inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

Atractylenolide I

Atractylenolide I is the major sesquiterpenoid of the rhizome of A. macrocephala and shows a wide spectrum of pharmacological activities such as antiinflammatory, digestion promoting, and antioxidant effects.

NQDI-1

NQDI 1, an inhibitor of ASK1(apoptosis signal-regulating kinase 1), attenuates acute ischemic renal injury by modulating oxidative stress and cell death.

VLX1570

VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.

CPI-455 HCl

CPI-455 is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

MKC-3946

MKC3946 is a potent and soluble IRE1α endoribonuclease domain inhibitor which triggered modest growth inhibition in multiple myeloma cell lines, without toxicity in normal mononuclear cells.

Fatostatin HBr

Fatostatin is an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.

SQ22536

SQ22536 is an inhibitor of adenylyl cyclase with an IC50 of 1.4 μM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.

CCF642

CCF642 is a novel PDI-inhibiting compound with antimyeloma activity.

IMR-1

IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 26 μM.

Shikonin

Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay.

SHP099 HCl

SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with an IC50 value of 0.071 μM and shows no activity against SHP1.

FCCP

FCCP is a potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.

Tomivosertib (eFT-508)

eFT-508 (eFT508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth.