SKLB-11A is a selective, first-in-class allosteric activator of SIRT3 that binds with a Kd of 4.7 μM and enhances its deacetylase activity with EC50 of 21.95 μM. It improves cardiac function and alleviates myocardial damage in vivo.

SKLB-11A is a selective, first-in-class allosteric activator of SIRT3 that binds with a Kd of 4.7 μM and enhances its deacetylase activity with EC50 of 21.95 μM. It improves cardiac function and alleviates myocardial damage in vivo.

CP-100356 hydrochloride is an orally active dual inhibitor of MDR1 (P-gp) and BCRP, with IC50 of ∼0.5 µM for MDR1-mediated calcein-AM transport inhibition and ∼1.5 µM for BCRP-mediated prazosin transport inhibition. It is also a weak inhibitor of OATP1B1 (IC50 ∼ 66 µM).

CP-100356 hydrochloride is an orally active dual inhibitor of MDR1 (P-gp) and BCRP, with IC50 of ∼0.5 µM for MDR1-mediated calcein-AM transport inhibition and ∼1.5 µM for BCRP-mediated prazosin transport inhibition. It is also a weak inhibitor of OATP1B1 (IC50 ∼ 66 µM).

SKLB-11A is a selective, first-in-class allosteric activator of SIRT3 that binds with a Kd of 4.7 μM and enhances its deacetylase activity with EC50 of 21.95 μM. It improves cardiac function and alleviates myocardial damage in vivo.

Ebio1 is a subtype-selective activator of the voltage-gated potassium channel KCNQ2 that enhances conductance through a unique twist-to-open mechanism. It induces conformational changes in the S6 helix, increasing channel activity at a saturating voltage (+50 mV).

CP-100356 hydrochloride is an orally active dual inhibitor of MDR1 (P-gp) and BCRP, with IC50 of ∼0.5 µM for MDR1-mediated calcein-AM transport inhibition and ∼1.5 µM for BCRP-mediated prazosin transport inhibition. It is also a weak inhibitor of OATP1B1 (IC50 ∼ 66 µM).

CP-100356 hydrochloride is an orally active dual inhibitor of MDR1 (P-gp) and BCRP, with IC50 of ∼0.5 µM for MDR1-mediated calcein-AM transport inhibition and ∼1.5 µM for BCRP-mediated prazosin transport inhibition. It is also a weak inhibitor of OATP1B1 (IC50 ∼ 66 µM).

Ebio1 is a subtype-selective activator of the voltage-gated potassium channel KCNQ2 that enhances conductance through a unique twist-to-open mechanism. It induces conformational changes in the S6 helix, increasing channel activity at a saturating voltage (+50 mV).

Ebio1 is a subtype-selective activator of the voltage-gated potassium channel KCNQ2 that enhances conductance through a unique twist-to-open mechanism. It induces conformational changes in the S6 helix, increasing channel activity at a saturating voltage (+50 mV).