fasudil

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Fasudil mesylate (HA-1077; AT877) is a nonspecific, orally active inhibitor of RhoA ROCK, exhibiting additional inhibitory effects on protein kinases with a K i of 0.33 μM for ROCK1. It shows IC 50 values of 0.158 μM for ROCK2, and 4.58 μM, 12.30 μM, and 1.650 μM for PKA, PKC, and PKG, respectively. Furthermore, Fasudil mesylate acts as a potent Ca 2+ channel antagonist and vasodilator, enhancing its pharmacological profile [1] [2] [3] [4] [5] [6].

Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3].

Fasudil hydrochloride hydrate is an HCl salt of Fasudil -- a Rho-kinase (ROCK) inhibitor that has been shown to be effective in hindering the development of mature Cerebral Cavernous Malformation (CCM) lesions as well as reducing portal venous pressure in cirrhotic rats.

Fasudil hydrochloride semihydrate is a useful organic compound for research related to life sciences and the catalog number is T64582.

Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) is a ROCK1 2 inhibitor (IC50s: 0.73 0.72 μM).

Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).

ROCK2-IN-5, a compound integrating structural elements from the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids, exhibits a favorable multitarget profile and tolerability. It shows potential for research in Amyotrophic Lateral Sclerosis (ALS) associated with a SOD1 mutation.

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

Olcorolimus inhibits single allergen-induced allergic inflammation such as eosinophilic and lymphocytic infiltration and mRNA expression for interleukin (IL)-4 and IL-5