T6321

Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3/2/1 (IC50=1/20/112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.

CDK7-IN-15 (Compound 8) is an effective CDK7 inhibitor for studying cancers associated with transcriptional dysregulation.

Everafenib is a potent BRAF inhibitor that crosses the blood-brain barrier and also inhibits the MAPK pathway. Everafenib inhibits the activity of a range of V600EBRAF melanoma cell lines (IC50: 2-10 nM) and is more effective than Dabrafenib and Vemurafenib. Everafenib was effective in extending the number of days of survival in a mouse model of intracranial metastatic melanoma.

AKT-IN-10 is a potent AKT inhibitor with research potential in breast and prostate cancers. It targets protein kinase B (PKB, also known as AKT), a key component of the PI3K/AKT/mTOR signaling pathway that is crucial for cell growth, survival, differentiation, and metabolism.

β-catenin-IN-3 is a selective and potent β-catenin inhibitor (KD: 54.96 nM) that targets a cryptic regulatory site of β-catenin and significantly reduces the viability of β-catenin-driven cancer cells.

Human enteropeptidase-IN-2 is a potent inhibitor of enteropeptidase (enteropeptidase) and can be used in anti-obesity studies.

Lomefloxacin (SC47111A) aspartate is a broad-spectrum quinolone antibacterial agent used in studying respiratory tract, gastrointestinal, genitourinary, and ear, nose, and throat infections.

COX-2-IN-22 is a COX-2 inhibitor (IC50: 8.6 μM) that can cross the blood-brain barrier and also exhibits inhibitory effects on AChE (IC50: 2.8 μM), BChE (IC50: 6.3 μM), β-Secretase (IC50: 15.3 μM), LOX-5 (IC50: 13.9 μM) and DPPH ( IC50: 6.8 μM) showed inhibitory effects.

5-{8-[(3,4'-Difluoro[1,1'-biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-N-methylpyridine-2-carboxamide (1o) exhibited high in vitro potency and brain exposure, significantly reduced brain Aβ42 levels, showed no inhibitory effect on cytochrome p450 enzymes, and demonstrated excellent anti-cognitive deficits in AD model mice.

Encephalitic alphavirus-IN-1 inhibited the activity of Venezuelan equine encephalitis virus (VEEV) (EC50: 0.24 μM) and eastern equine encephalitis virus (EEEV) (EC50: 0.16 μM). encephalitic alphavirus-IN-1 was not significantly cytotoxic and exhibited strong plasma stability in mice.

Tofacitinib-13C3 is a carbon-13 labeled variant of Tofacitinib. Tofacitinib (T6321) acts as a JAK3/2/1 inhibitor, exhibiting IC50 values of 1 nM, 20 nM, and 112 nM, respectively.