製品番号: HY-10341A

Fasudil

(別名: HA-1077; AT877)

29 Cited Publications

カスタマーレビュー

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 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 is also a potent Ca²⁺ channel antagonist and vasodilator.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.98%
CAS 番号: 103745-39-7
分子式: C₁₄H₁₇N₃O₂S
分子量:291.37

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Fasudil 構造式

CAS 番号: 103745-39-7

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数量

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (29)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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)

ROCK アイソフォーム固有の製品をすべて表示 :

Calcium Channel アイソフォーム固有の製品をすべて表示 :

PKA アイソフォーム固有の製品をすべて表示 :

PKC アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HASMC	IC₅₀	1.3 μM Compound: Fasudil	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	[PMID: 33569941]
HEK293	IC₅₀	4 μM Compound: HA-1077	Inhibition of His-tagged human PRK2 expressed in HEK293 cells Inhibition of His-tagged human PRK2 expressed in HEK293 cells	[PMID: 10998351]
Sf9	IC₅₀	1.9 μM Compound: HA-1077	Inhibition of rat ROCK2 expressed in Sf9 cells Inhibition of rat ROCK2 expressed in Sf9 cells	[PMID: 10998351]
Sf9	IC₅₀	300 nM Compound: Fasudil	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	[PMID: 17018693]
Sf9	IC₅₀	5 μM Compound: HA-1077	Inhibition of His-tagged human MSK1 expressed in Sf9 cells Inhibition of His-tagged human MSK1 expressed in Sf9 cells	[PMID: 10998351]
U-937	IC₅₀	35 μM Compound: HA-1077	Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2 Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2	[PMID: 17084087]

体外実験

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.

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.

体内実験

Fasudil (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 (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 (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.

化学情報

CAS 番号 103745-39-7
性状 Solid
分子量 291.37
分子式 C₁₄H₁₇N₃O₂S
Color Off-white to light yellow
SMILES

O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O
別名

HA-1077; AT877
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (29)

All WBIn Vivo Efficacy StudyCell Imaging/Staining

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Journal Impact Factor

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

Nanoparticles reach metastatic tumours via enhanced permeability of adjacent vessels. [Abstract]

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

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
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.
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.
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

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

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
Transl Neurosci

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

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

2025 Dec 2.
SSRN

2023 Feb 24.

溶剤 & 溶解度

体外:

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)

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

3.4321 mL

17.1603 mL

34.3206 mL

5 mM

0.6864 mL

3.4321 mL

6.8641 mL

10 mM

0.3432 mL

1.7160 mL

3.4321 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.33 mg/mL (11.43 mM); Clear solution

This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[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

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

Fasudil

29 Cited Publications

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Fasudil

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MedChemExpress（MCE）の使用を引用している文献 Fasudil

ROCK アイソフォーム固有の製品をすべて表示

Calcium Channel アイソフォーム固有の製品をすべて表示

PKA アイソフォーム固有の製品をすべて表示

PKC アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (29)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Fasudil 関連分類

HY-10341A 関連分類