Fasudil
Based on 29 publication(s) in Google Scholar
Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+ channel antagonist and vasodilator.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 103745-39-7
- Formula: C14H17N3O2S
- Molecular Weight:291.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Fasudil
More- Mol Cancer. 2026 Apr 2;25(1):130. [Abstract]
- Nat Nanotechnol. 2026 Jun;21(6):880-891. [Abstract]
- Cell Mol Immunol. 2023 Apr;20(4):351-364. [Abstract]
- Cell Stem Cell. 2025 Apr 3;32(4):581-597.e11. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Exp Clin Cancer Res. 2020 Jun 16;39(1):113. [Abstract]
- Int J Biol Sci. 2024 Jan 12;20(3):897-915. [Abstract]
- NPJ Precis Oncol. 2025 Nov 26;9(1):391. [Abstract]
- Neural Regen Res. 2021 Dec;16(12):2512-2520. [Abstract]
- Clin Transl Med. 2022 Oct;12(10):e1036. [Abstract]
- Clin Transl Med. 2022 Jul;12(7):e961. [Abstract]
- Br J Cancer. 2023 May;128(10):1941-1954. [Abstract]
- Aging Cell. 2025 Jan;24(1):e14366. [Abstract]
- Aging Cell. 2024 Sep;23(9):e14209. [Abstract]
- Biochem Pharmacol. 2025 Jul:237:116933. [Abstract]
- Inflammopharmacology. 2023 Aug;31(4):2037-2047. [Abstract]
- Eur J Pharmacol. 2024 Jul 15:975:176640. [Abstract]
- Diabetol Metab Syndr. 2025 Oct 3;17(1):374. [Abstract]
- Sci Rep. 2018 Feb 6;8(1):2477. [Abstract]
- Cell Signal. 2026 Feb:138:112275. [Abstract]
- J Cereb Blood Flow Metab. 2025 Jun;45(6):1191-1202. [Abstract]
- iScience. 2026 Feb 23;29(3):115122. [Abstract]
- Metab Brain Dis. 2025 Jan 7;40(1):91. [Abstract]
- J Pharm Pharmacol. 2021 Jul 7;73(8):1118-1127. [Abstract]
- Adipocyte. 2019 Dec;8(1):114-124. [Abstract]
- Biomed Rep. 2015 May;3(3):361-364. [Abstract]
- Transl Neurosci. 2020 Apr 20;11(1):75-86. [Abstract]
- Preprints. 2025 Dec 2.
- SSRN. 2023 Feb 24.
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WB
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In Vivo Efficacy Study
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Cell Imaging/Staining
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WB
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WB
All Calcium Channel Isoforms
More
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
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| HASMC | IC50 |
1.3 μM
Compound: Fasudil
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Antiproliferative activity against human HASMC cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
Antiproliferative activity against human HASMC cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
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[PMID: 33569941] |
| HEK293 | IC50 |
4 μM
Compound: HA-1077
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Inhibition of His-tagged human PRK2 expressed in HEK293 cells
Inhibition of His-tagged human PRK2 expressed in HEK293 cells
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[PMID: 10998351] |
| Sf9 | IC50 |
1.9 μM
Compound: HA-1077
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Inhibition of rat ROCK2 expressed in Sf9 cells
Inhibition of rat ROCK2 expressed in Sf9 cells
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[PMID: 10998351] |
| Sf9 | IC50 |
300 nM
Compound: Fasudil
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Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
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[PMID: 17018693] |
| Sf9 | IC50 |
5 μM
Compound: HA-1077
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Inhibition of His-tagged human MSK1 expressed in Sf9 cells
Inhibition of His-tagged human MSK1 expressed in Sf9 cells
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[PMID: 10998351] |
| U-937 | IC50 |
35 μM
Compound: HA-1077
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Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
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[PMID: 17084087] |
Fasudil (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells[4]. Fasudil (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells[4]. Fasudil (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rat HSCs and human HSC-derived TWNT-4 cells
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Concentration:50 μM; 100 μM
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Incubation Time:24 hours
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Result:Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively.
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Cell Line:Rat HSCs and human HSC-derived TWNT-4 cells
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Concentration:25 μM; 50 μM; 100 μM
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Incubation Time:24 hours
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Result:Reduced the expression of type I collagen, a-SMA, and TIMP-1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Myocardial ischemia and reperfusion in rat (250-300 g)[5]
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Dosage:10 mg/kg
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Administration:Intravenous injection; 1 h before operation
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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.
Chemical Information
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CAS No. 103745-39-7
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Appearance Solid
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Molecular Weight 291.37
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Formula C14H17N3O2S
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Color Off-white to light yellow
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SMILES
O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O
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Synonyms
HA-1077; AT877
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (29)
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Journal Impact Factor
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Most Recent
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Mol Cancer
ROCK1 inhibition primes anti-tumor immunity in EGFR-mutant NSCLC by triggering PD-L1 degradation mediated by SMURF2. [Abstract]2026 Apr 2;25(1):130. PMID: 41928228 -
Nat Nanotechnol
2026 Jun;21(6):880-891. PMID: 42286217 -
Cell Mol Immunol
A SARS-CoV-2-specific CAR-T-cell model identifies felodipine, fasudil, imatinib, and caspofungin as potential treatments for lethal COVID-19. [Abstract]2023 Apr;20(4):351-364. PMID: 36864189 -
Cell Stem Cell
Mechano-oncogenic cytoskeletal remodeling drives leukemic transformation with mitochondrial vesicle-mediated STING activation. [Abstract]2025 Apr 3;32(4):581-597.e11. PMID: 39986274 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Exp Clin Cancer Res
3,3'-Diindolylmethane modulates aryl hydrocarbon receptor of esophageal squamous cell carcinoma to reverse epithelial-mesenchymal transition through repressing RhoA/ROCK1-mediated COX2/PGE2 pathway. [Abstract]2020 Jun 16;39(1):113. PMID: 32546278 -
Int J Biol Sci
2024 Jan 12;20(3):897-915. PMID: 38250154 -
NPJ Precis Oncol
GLMP promotes EGFR-TKI resistance by activating autophagy and RhoA pathway in non-small cell lung cancer. [Abstract]2025 Nov 26;9(1):391. PMID: 41298761 -
Neural Regen Res
Environmental enrichment combined with fasudil promotes motor function recovery and axonal regeneration after stroke. [Abstract]2021 Dec;16(12):2512-2520. PMID: 33907042 -
Clin Transl Med
Inhibition of ROCK ameliorates pulmonary fibrosis by suppressing M2 macrophage polarisation through phosphorylation of STAT3. [Abstract]2022 Oct;12(10):e1036. PMID: 36178087 -
Clin Transl Med
Functional genomic analysis of epithelioid sarcoma reveals distinct proximal and distal subtype biology. [Abstract]2022 Jul;12(7):e961. PMID: 35839307 -
Br J Cancer
Functional genomics of human clear cell sarcoma: genomic, transcriptomic and chemical biology landscape for clear cell sarcoma. [Abstract]2023 May;128(10):1941-1954. PMID: 36959380 -
Aging Cell
Hippocampal Nogo66-NgR1 signaling activation restricts postsynaptic assembly in aged mice with postoperative neurocognitive disorders. [Abstract]2025 Jan;24(1):e14366. PMID: 39412367 -
Aging Cell
Sevoflurane-induced overexpression of extrasynaptic α5-GABAAR via the RhoA/ROCK2 pathway impairs cognitive function in aged mice. [Abstract]2024 Sep;23(9):e14209. PMID: 38825816
Fasudil purchased from MedChemExpress. Usage Cited in: Aging Cell. 2024 Sep;23(9):e14209. [Abstract]
Western blot images of ROCK2, radixin, and p-ERM bands in total protein samples and α5-GABAAR bands in membrane protein samples. β-Actin and NKA were used as total protein and membrane protein loading controls, respectively. Total proteins and membrane proteins were extracted from the mouse hippocampus. Aged C57BL/6 mice (female, 18–19 months old), Fasudil Hydrochloride (20 mg/kg/day; ip) for 7 days before anesthesia.
Fasudil purchased from MedChemExpress. Usage Cited in: Aging Cell. 2024 Sep;23(9):e14209. [Abstract]
Escape latency in the training stage. Aged C57BL/6 mice (female, 18–19 months old), Fasudil Hydrochloride (20 mg/kg/day; ip) for 7 days before anesthesia.
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Biochem Pharmacol
The dual targeting effects of KD025 on casein kinase 2 and ROCK2 in a mouse model of diet-induced obesity. [Abstract]2025 Jul:237:116933. PMID: 40210126 -
Inflammopharmacology
Diosmetin alleviates acute lung injury caused by lipopolysaccharide by targeting barrier function. [Abstract]2023 Aug;31(4):2037-2047. PMID: 37074600 -
Eur J Pharmacol
Fasudil attenuates oxidative stress-induced partial epithelial-mesenchymal transition of tubular epithelial cells in hyperuricemic nephropathy via activating Nrf2. [Abstract]2024 Jul 15:975:176640. PMID: 38750716 -
Diabetol Metab Syndr
THBS1 regulates the function and insulin sensitivity of HTR8/SVneo cells treated with high glucose through the RhoA/ROCK1 signaling pathway. [Abstract]2025 Oct 3;17(1):374. PMID: 41044623 -
Sci Rep
Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells. [Abstract]2018 Feb 6;8(1):2477. PMID: 29410516
Fasudil purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Feb 6;8(1):2477. [Abstract]
3T3-L1 cells were differentiated by incubation in DMI with KD025, Y-27632, or Fasudil Hydrochloride (fasudil; 10 μM) as indicated, and stained with Oil Red O on day 8.
Fasudil purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Feb 6;8(1):2477. [Abstract]
3T3-L1 pre-adipocytes were treated with KD025 (7 µM),Y-27632 (10µM), Fasudil Hydrochloride (fasudil ; 10 µM), H-1152P (3 µM), or SR3677 (5 µM) for one day.
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Cell Signal
RhoA/ROCK1 aggravates transverse aortic constriction-induced atrial fibrillation by enhancing NF-κBp65/CCL2 signaling pathway. [Abstract]2026 Feb:138:112275. PMID: 41317932 -
J Cereb Blood Flow Metab
Isoform-selective and non-selective rho-kinase inhibitors do not affect collagenase-induced intracerebral hemorrhage outcomes in mice: Influence of sex and circadian cycle. [Abstract]2025 Jun;45(6):1191-1202. PMID: 39763388 -
iScience
2026 Feb 23;29(3):115122. PMID: 41852725 -
Metab Brain Dis
Ginkgo biloba extract mediates HT22 cell proliferation and migration after oxygen-glucose deprivation/reoxygenation via regulating RhoA-ROCK2 signalling pathway. [Abstract]2025 Jan 7;40(1):91. PMID: 39775993 -
J Pharm Pharmacol
Fasudil alleviated insulin resistance through promotion of proliferation, attenuation of cell apoptosis and inflammation and regulation of RhoA/Rho kinase/insulin/nuclear factor-κB signalling pathway in HTR-8/SVneo cells. [Abstract]2021 Jul 7;73(8):1118-1127. PMID: 33779714 -
Adipocyte
KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells. [Abstract]2019 Dec;8(1):114-124. PMID: 30860936 -
Biomed Rep
Inhibiting Rho kinase 2 reduces memory dysfunction in adult rats exposed to sevoflurane at postnatal days 7-9. [Abstract]2015 May;3(3):361-364. PMID: 26137236
Fasudil purchased from MedChemExpress. Usage Cited in: Biomed Rep. 2015 May;3(3):361-364. [Abstract]
RhoA and ROCK2 upregulation in the rat hippocampus is involved in memory dysfunction induced by postnatal exposure of Sevoflurane. The expression of RhoA, ROCK2 and cleaved caspase-3 (Cl-Csp3) in the hippocampus of the S3 group significantly increased, compared to that of the C group (P<0.05). There is no difference of the level of RhoA, ROCK2 and Cl-Csp3 between the C and S1 groups (P>0.05). ROCK2 inhibitor Fasudil hydrochloride in the F group clearly decreases the expression of ROCK2 and Cl-Cs
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Transl Neurosci
2020 Apr 20;11(1):75-86. PMID: 33335751 -
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Solvent & Solubility
DMSO : 33.33 mg/mL (114.39 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.33 mg/mL (11.43 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.33 mg/mL (11.43 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Chen M, et al. Fasudil and its analogs: a new powerful weapon in the long war against central nervous system disorders? Expert Opin Investig Drugs. 2013 Apr;22(4):537-50. [Content Brief]
[2]. Huang XN, et al. The effects of fasudil on the permeability of the rat blood-brain barrier and blood-spinal cordbarrier following experimental autoimmune encephalomyelitis. J Neuroimmunol. 2011 Oct 28;239(1-2):61-7. [Content Brief]
[3]. Uehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 1997 Oct 30;389(6654):990-4. [Content Brief]
[4]. Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38. [Content Brief]
[5]. Zhang J, et al. Inhibition of the activity of Rho-kinase reduces cardiomyocyte apoptosis in heart ischemia/reperfusion via suppressing JNK-mediated AIF translocation. Clin Chim Acta. 2009 Mar;401(1-2):76-80. [Content Brief]
[6]. Sun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180(1-2):126-34. Epub 2006 Sep 22. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4321 mL | 17.1603 mL | 34.3206 mL | 85.8016 mL |
| 5 mM | 0.6864 mL | 3.4321 mL | 6.8641 mL | 17.1603 mL | |
| 10 mM | 0.3432 mL | 1.7160 mL | 3.4321 mL | 8.5802 mL | |
| 15 mM | 0.2288 mL | 1.1440 mL | 2.2880 mL | 5.7201 mL | |
| 20 mM | 0.1716 mL | 0.8580 mL | 1.7160 mL | 4.2901 mL | |
| 25 mM | 0.1373 mL | 0.6864 mL | 1.3728 mL | 3.4321 mL | |
| 30 mM | 0.1144 mL | 0.5720 mL | 1.1440 mL | 2.8601 mL | |
| 40 mM | 0.0858 mL | 0.4290 mL | 0.8580 mL | 2.1450 mL | |
| 50 mM | 0.0686 mL | 0.3432 mL | 0.6864 mL | 1.7160 mL | |
| 60 mM | 0.0572 mL | 0.2860 mL | 0.5720 mL | 1.4300 mL | |
| 80 mM | 0.0429 mL | 0.2145 mL | 0.4290 mL | 1.0725 mL | |
| 100 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8580 mL |