Biologically Active Small Molecules

A negative allosteric modulator of CaSR that blocks calcium-mediated activation (IC₅₀ = 0.39 &microM) attenuates the activation of CaSR by calcimimetics.

A negative allosteric modulator of CaSR that blocks calcium-mediated activation (IC₅₀ = 0.39 &microM) attenuates the activation of CaSR by calcimimetics.

A phenylalkylamine calcimimetic that facilitates the activation of CaSR, a GPCR that triggers PI-intracellular Ca2+ signaling stimulates PI hydrolysis and proliferation through human CaSR (pEC₅₀ values are 6.9 and 7.

A phenylalkylamine calcimimetic that facilitates the activation of CaSR, a GPCR that triggers PI-intracellular Ca2+ signaling stimulates PI hydrolysis and proliferation through human CaSR (pEC₅₀ values are 6.9 and 7.

A phenylalkylamine calcimimetic that facilitates the activation of CaSR, a GPCR that triggers PI-intracellular Ca2+ signaling stimulates PI hydrolysis and proliferation through human CaSR (pEC₅₀ values are 6.9 and 7.

A phenylalkylamine calcimimetic that facilitates the activation of CaSR, a GPCR that triggers PI-intracellular Ca2+ signaling stimulates PI hydrolysis and proliferation through human CaSR (pEC₅₀ values are 6.9 and 7.

An inhibitor of CaM, inhibiting CaM-dependent phosphodiesterase and CaM-induced activation of erythrocyte calcium-transporting ATPase (IC₅₀ = 0.15 and 0.

A synthetic tripeptide aldehyde that acts as a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM) cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM) prevents the degradation of I&kappaB&alpha

A synthetic tripeptide aldehyde that acts as a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM) cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM) prevents the degradation of I&kappaB&alpha

A synthetic tripeptide aldehyde that acts as a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM) cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM) prevents the degradation of I&kappaB&alpha

A synthetic tripeptide aldehyde that acts as a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM) cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM) prevents the degradation of I&kappaB&alpha

A cell permeable, peptide aldehyde inhibitor of calpain I (Ki = 120 nM), calpain II (Ki = 230 nM), cathepsin B (Ki = 100 nM), and cathepsin L (Ki = 0.6 nM).