Fasudil, Monohydrochloride Salt is a cell-permeable, selective ROCK inhibitor which induces neuroprotection in vitro. Studies suggest that when acting as a ROCK inhibitor, Fasudil reduces neutrophil transendothelial migration by diminishing cytoskeletal rearrangement of endothelial cells. In addition, Fasudil significantly protects against MeHg-induced axonal degeneration and apoptotic cell death in cultured cortical neurons. Alternate studies show that Fasudil plays an important role in osteoblastic differentiation of stromal cells via increasing the mRNA expression of collagen-I, osteocalcin, and bone morphogenetic protein-2 (BMP-2). Furthermore, noggin, a BMP-2 antagonist can reverse the effects of Fasudil induced mRNA expression of collagen-I and osteocalcin. Upon inhibition of Rho-kinase, Fasudil significantly stimulates FGF-2-induced accumulation of vascular endothelial growth factor (VEGF). Fasudil, Monohydrochloride Salt is an inhibitor of cGKI, MSK1, PKA, PRK2, Rock-2, AMPK, CaMKII, Polycystin-1 and Rsk-1.
1. Kanazawa, I., et al. 2010. Endocr. J. 57: 415-421. PMID: 20154408 2. Ding, J., et al. 2010. J. Neurochem. 114: 1619-1629. PMID: 20882700 3. Li, Y., et al. 2010. Med. Sci. Monit. 16: BR112-BR118. PMID: 20357711 4. Fujimura, M., et al. 2011. Toxicol. Appl. Pharmacol. 250: 1-9. PMID: 20869980
Soluble in water (200 mg/mL), and DMSO (95 mg/mL). Insoluble in ethanol.
Store at -20° C
506.2° C at 760 mmHg (Predicted)
n20D ~1.62 (Predicted)
Rho-associated Kinase II: IC50 = 1.9 µM; Protein Kinase C-Related Kinase 2: IC50 = 4 µM; Mitogen- and Stress-Activated Protein Kinase 1: IC50 = 5 µM; Mitogen Activated Protein Kinase-Activated Protein Kinase 1b: IC50 = 5 µM; Rho-associated Kinase : IC50 = 10.7 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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ChengCheng, YT. et al. (PubMed 26313863) evaluated whether ROCK is involved in embryonic stem (ES) cell differentiation into cardiac and hematopoietic lineages by utilizing ROCK inhibitor Fasudil on murine ES. ROCK inhibition resulted in a drastic change in colony morphology accompanied by loss of hematopoietic markers (GATA-1, CD41 and -Major) and expressed markers of cardiac lineages (GATA-4, Isl-1, Tbx-5, Tbx-20, MLC-2a, MLC-2v, -MHC, cTnI and cTnT) in murine ES. -SCBT Publication Review
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