Fasudil mesylate
Based on 29 publication(s) in Google Scholar
Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active 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 mesylate is also a potent Ca2+ channel antagonist and vasodilator.
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- CAS No.: 1001206-62-7
- Formule: C15H21N3O5S2
- Masse moléculaire:387.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Fasudil mesylate
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 Jun 2:e14209. [Abstract]
- Biochem Pharmacol. 2025 Apr 8:116933. [Abstract]
- Inflammopharmacology. 2023 Aug;31(4):2037-2047. [Abstract]
- Eur J Pharmacol. 2024 May 13:975:176640. [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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Activité biologique
Ki: 0.33 μM (ROCK1)[1]
IC50: 0.158 μM (ROCK2), 4.58 μM (PKA), 12.30 μM (PKC), 1.650 μM (PKG)[1]
Chemical Information
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CAS No. 1001206-62-7
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Masse moléculaire 387.47
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Formule C15H21N3O5S2
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SMILES
CS(O)(=O)=O.O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O
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Synonyms
HA-1077 mesylate; AT-877 mesylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
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 Jun 2:e14209. PMID: 38825816
Fasudil mesylate 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 mesylate 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.
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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 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 -
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 mesylate 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 mesylate 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 mesylate 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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Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fasudil mesylate Related Classifications
HY-10341D Related Classifications
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