| Field | Specification |
|---|---|
| Target | |
| Alternative names | HA-1077; AT877 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C14H17N3O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Fasudil, also known as HA-1077 or AT877, is a nonspecific RhoA/ROCK inhibitor that also inhibits other protein kinases, with a Ki of 0.33 μM for ROCK1 and IC50 values of 0.158 μM for ROCK2, 4.58 μM for PKA, 12.30 μM for PKC, and 1.650 μM for PKG. It is also a potent Ca2+ channel antagonist and vasodilator[1][2][3]. It is supplied as an off-white to light yellow solid (C14H17N3O2S, MW 291.37) at 99.98% purity.
Physical & Chemical Properties
| CAS Number | 103745-39-7 |
|---|---|
| Molecular Formula | C14H17N3O2S |
| Molecular Weight | 291.37 g/mol |
| Purity | 99.98% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O |
| Target | p160ROCK, ROCK2, PKA, PKC, PKG |
| Signaling Pathway | Cell Cycle/DNA Damage; TGF-beta/Smad; Stem Cell/Wnt; Cytoskeleton; Neuronal Signaling; Membrane Transporter/Ion Channel; Autophagy; Epigenetics |
| Solubility | In Vitro: DMSO: 33.33 mg/mL (114.39 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
p160ROCK 0.33 μM (Ki) |
ROCK2 0.158 μM (IC50) |
PKA 4.58 μM (IC50) |
PKC 12.3 μM (IC50) |
PKG 1.65 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 33.33 mg/mL (114.39 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 3.33 mg/mL (11.43 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3.33 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (33.3 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 3.33 mg/mL (11.43 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3.33 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (33.3 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 3.33 mg/mL (11.43 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3.33 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (33.3 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Rat hepatic stellate cells (HSCs) and human TWNT-4 cells derived from HSCs, when treated with Fasudil (100 μM), show inhibited cell spreading, stress fiber formation, and α-SMA expression, along with concomitant suppression of cell growth[4]. Western blotting shows that Fasudil (50-100 μM; 24 hours) blocks phosphorylation of ERK1/2, JNK, and p38 induced by LPA (lysophosphatidic acid) in rat HSCs and in TWNT-4 cells derived from human HSCs[4]. In TWNT-4 cells derived from human HSCs, Fasudil (25-100 μM; 24 hours) suppresses collagen and TIMP transcription and stimulates MMP-1 transcription[4].
Western Blot Analysis[4]
| Cell Line | Rat HSCs and human HSC-derived TWNT-4 cells |
|---|---|
| Concentration | 50 μM; 100 μM |
| Incubation Time | 24 hours |
| Result | Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively. |
RT-PCR[4]
| Cell Line | Rat HSCs and human HSC-derived TWNT-4 cells |
|---|---|
| Concentration | 25 μM; 50 μM; 100 μM |
| Incubation Time | 24 hours |
| Result | Reduced the expression of type I collagen, a-SMA, and TIMP-1. |
In Vivo
Fasudil (10 mg/kg; i.v.; 1 h before operation) shows protective effects on cardiovascular disease, reducing JNK activation and attenuating mitochondrial-nuclear translocation of AIF under ischemic injury[5]. At 50 mg/kg/d (i.p.), Fasudil suppresses acute and relapsing EAE (experimental autoimmune encephalomyelitis) that is induced by proteolipid protein PLP p139-151, reduces lymphocyte proliferation, downregulates interleukin (IL)-17, and markedly lowers the IFN-γ/IL-4 ratio[6]. In SJL/J mice, Fasudil (100 mg/kg/d; p.o.) significantly lowers the incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) and decreases inflammation, demyelination, axonal loss, and APP positivity in the spinal cord[6].
| Animal Model | Myocardial ischemia and reperfusion in rat (250-300 g)[5] |
|---|---|
| Dosage | 10 mg/kg |
| Administration | Intravenous injection; 1 h before operation |
| Result | Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus. Inhibited Rho-kinase activity, and reduced myocardial infarct size and heart cell apoptosis. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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GLMP promotes EGFR-TKI resistance by activating autophagy and RhoA pathway in non-small cell lung cancer. NPJ Precis Oncol 2025 Nov 26;9(1):391. PMID: 41298761
Environmental enrichment combined with fasudil promotes motor function recovery and axonal regeneration after stroke. Neural Regen Res 2021 Dec;16(12):2512-2520. PMID: 33907042
Inhibition of ROCK ameliorates pulmonary fibrosis by suppressing M2 macrophage polarisation through phosphorylation of STAT3. Clin Transl Med 2022 Oct;12(10):e1036. PMID: 36178087
