Fasudil

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CAS: 103745-39-7

Name:

Fasudil

Other names:

HA-1077; AT 877; HA1077; Fasudil [INN]; HA 1077; (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE; Fasudilum [INN-Latin]

HA-1077 dihydrochloride has been shown to be a vasodilating agent as well as a potent inhibitor of Rock-2 (Rho-associated Kinase II), cGKI (cGMP-dependent protein kinase), PKA (cAMP-dependent protein kinase), MYLK, and CaMKII. Rho kinase signaling pathways are thought to cause invasion, migration, and proliferation of certain cells. Studies have shown this compound can also inhibit myosin light chain kinase in vitro and suppress cell rounding by myosin light chain phosphorylation. Mechanistic experiments report that HA-1077 inhibits vascular smooth muscle contraction by acting as a calcium channel protein inhibitor. HA-1077 dihydrochloride is an inhibitor of MSK1, PKC, PRK2 and Rsk-2.

Interactions

Description

UniProt ID

Protein: Myosin light chain kinase, smooth muscle, Gene: MYLK
Protein: Myosin light chain kinase 2, skeletal/cardiac muscle, Gene: MYLK2
Protein: Myosin light chain kinase 3, Gene: MYLK3
Protein: cAMP-dependent protein kinase catalytic subunit alpha, Gene: PRKACA
Gene: PRKACB
Protein: cAMP-dependent protein kinase catalytic subunit gamma, Gene: PRKACG
Protein: Protein kinase C alpha type, Gene: PRKCA
Protein: Protein kinase C delta type, Gene: PRKCD
Protein: Protein kinase C epsilon type, Gene: PRKCE
Protein: Protein kinase C gamma type, Gene: PRKCG

Toxicity

oral LD50 [mouse] mg/kg
Unavailable
oral LD50 [rat] mg/kg
Unavailable
oral LD50 [rabbit] mg/kg
Unavailable

Effects on organism

Anti Inflammation
Anti Cancer
Anti Amiloid
Anti Atherogenic
Anti Diabetic
Neuroprotective
Cardioprotective
Antibacterial

No

Antifungal

No

Antiviral

No

Longevity mechanisms activation

Stress Resistance

Suppression of aging mechanisms

No data

Relation to biomarkers of Aging

Improves learning and working memory

19170447

Relation to aging associated genes

PRKCAPRKCAPRKCD

Experimental conditions

Not available

Life Extension

Mean LS (%)
14.5
Median LS (%)
Mortality rate derease (%)
Max LS (%)
Cell CLS
Cell RLS

Concentration wth maximum effect

More info about experiment

22363408
Opposite effectNo