Cat. No.: HY-10341C

Fasudil dihydrochloride

(Synonyms: HA-1077 dihydrochloride; AT-877 dihydrochloride)

27 Cited Publications

Customer Review

Based on 27 publication(s) in Google Scholar

Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i 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 dihydrochloride is also a potent Ca²⁺ channel antagonist and vasodilator.

For research use only. We do not sell to patients.

Purity: 99.98%
CAS No.: 203911-27-7
Formula: C₁₄H₁₉Cl₂N₃O₂S
Molecular Weight:364.29

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Fasudil dihydrochloride Chemical Structure

CAS No.: 203911-27-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (27)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

PKA

4.58 μM (IC₅₀)

PKC

12.3 μM (IC₅₀)

PKG

1.65 μM (IC₅₀)

p160ROCK

0.33 μM (Ki)

ROCK2

0.158 μM (IC₅₀)

All Calcium Channel Isoforms :

All ROCK Isoforms :

All PKA Isoforms :

All PKC Isoforms :

All HIV Isoforms :

In Vitro

Fasudil dihydrochloride (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 dihydrochloride (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 dihydrochloride (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.

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 dihydrochloride (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury^[5].
Fasudil dihydrochloride (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio^[6].
Fasudil dihydrochloride (100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 203911-27-7
Appearance Solid
Molecular Weight 364.29
Formula C₁₄H₁₉Cl₂N₃O₂S
Color White to off-white
SMILES

O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O.[H]Cl.[H]Cl
Synonyms

HA-1077 dihydrochloride; AT-877 dihydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (27)

All WBIn Vivo Efficacy StudyCell Imaging/Staining

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Journal Impact Factor

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
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
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

Angiogenic and Fibrogenic Dual-effect of Gremlin1 on Proliferative Diabetic Retinopathy. [Abstract]

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
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 Jun 2:e14209. PMID: 38825816

Fasudil dihydrochloride purchased from MedChemExpress. Usage Cited in: Aging Cell. 2024 Jun 2: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 dihydrochloride purchased from MedChemExpress. Usage Cited in: Aging Cell. 2024 Jun 2: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.
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
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
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
Biochem Pharmacol

The dual targeting effects of KD025 on casein kinase 2 and ROCK2 in a mouse model of diet-induced obesity. [Abstract]

2025 Apr 8:116933. 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 May 13:975:176640. PMID: 38750716
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

A stress-responsive neurovascular axis shapes skin immune accessibility. [Abstract]

2026 Feb 23;29(3):115122. PMID: 41852725
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 dihydrochloride 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 dihydrochloride 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.
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
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
Transl Neurosci

Hydrochloride fasudil attenuates brain injury in ICH rats. [Abstract]

2020 Apr 20;11(1):75-86. PMID: 33335751
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 dihydrochloride 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
Preprints

2025 Dec 2.
SSRN

2023 Feb 24.

Solvent & Solubility

In Vitro:

H₂O : ≥ 100 mg/mL (274.51 mM)

DMSO : 20.83 mg/mL (57.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7451 mL

13.7253 mL

27.4507 mL

5 mM

0.5490 mL

2.7451 mL

5.4901 mL

10 mM

0.2745 mL

1.3725 mL

2.7451 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	2.7451 mL	13.7253 mL	27.4507 mL	68.6266 mL
	5 mM	0.5490 mL	2.7451 mL	5.4901 mL	13.7253 mL
	10 mM	0.2745 mL	1.3725 mL	2.7451 mL	6.8627 mL
	15 mM	0.1830 mL	0.9150 mL	1.8300 mL	4.5751 mL
	20 mM	0.1373 mL	0.6863 mL	1.3725 mL	3.4313 mL
	25 mM	0.1098 mL	0.5490 mL	1.0980 mL	2.7451 mL
	30 mM	0.0915 mL	0.4575 mL	0.9150 mL	2.2876 mL
	40 mM	0.0686 mL	0.3431 mL	0.6863 mL	1.7157 mL
	50 mM	0.0549 mL	0.2745 mL	0.5490 mL	1.3725 mL
H₂O	60 mM	0.0458 mL	0.2288 mL	0.4575 mL	1.1438 mL
	80 mM	0.0343 mL	0.1716 mL	0.3431 mL	0.8578 mL
	100 mM	0.0275 mL	0.1373 mL	0.2745 mL	0.6863 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Fasudil dihydrochloride

27 Cited Publications

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Fasudil dihydrochloride

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Publications Citing Use of MedChemExpress (MCE) Fasudil dihydrochloride

All Calcium Channel Isoforms

All ROCK Isoforms

All PKA Isoforms

All PKC Isoforms

All HIV Isoforms

Biological Activity

Chemical Information

Publications (27)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Fasudil dihydrochloride Related Classifications

Cat. No.: HY-10341C