Biologically Active Small Molecules

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

Selectively inhibits MEK1/2 potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation (IC50s = 10 and 18.2 nM, respectively) 30 mg/kg reduced tumor growth significantly in mice

Selectively inhibits MEK1/2 potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation (IC50s = 10 and 18.2 nM, respectively) 30 mg/kg reduced tumor growth significantly in mice

Selectively inhibits MEK1/2 potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation (IC50s = 10 and 18.2 nM, respectively) 30 mg/kg reduced tumor growth significantly in mice

Selectively inhibits MEK1/2 potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation (IC50s = 10 and 18.2 nM, respectively) 30 mg/kg reduced tumor growth significantly in mice

An isoprenoid antibiotic and antiviral that suppresses PMA-induced invasion in renal carcinoma cells (IC₅₀ = ~10 &microM) by inhibiting the expression of MMP-9 profoundly increases the expression of p53 by increasing protein stability

An isoprenoid antibiotic and antiviral that suppresses PMA-induced invasion in renal carcinoma cells (IC₅₀ = ~10 &microM) by inhibiting the expression of MMP-9 profoundly increases the expression of p53 by increasing protein stability

An ethyl analog of tacrolimus with potent immunosuppressant properties that prevents T-cell proliferation through initial binding to FKBP12, the principal mediator of FK506- and rapamycin-induced immunosuppression inhibits the enzymatic PPIase and

An ethyl analog of tacrolimus with potent immunosuppressant properties that prevents T-cell proliferation through initial binding to FKBP12, the principal mediator of FK506- and rapamycin-induced immunosuppression inhibits the enzymatic PPIase and

An ethyl analog of tacrolimus with potent immunosuppressant properties that prevents T-cell proliferation through initial binding to FKBP12, the principal mediator of FK506- and rapamycin-induced immunosuppression inhibits the enzymatic PPIase and