Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.

Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].

Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].

ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels.

RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), […]

RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), […]

Abequolixron (RGX-104) is a orally bioavailable liver X receptor agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

Abequolixron (RGX-104) is a orally bioavailable liver X receptor agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

Abequolixron (RGX-104) is a orally bioavailable liver X receptor agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.