Fasudil, Monohydrochloride SaltA selective ROCK inhibitor

Fasudil, Monohydrochloride Salt (CAS 105628-07-7)

Fasudil, Monohydrochloride Salt | CAS 105628-07-7 is rated 5.0 out of 5 by 1.
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Synonym: Eril; 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride
Application: A selective ROCK inhibitor
CAS Number: 105628-07-7
Purity: ≥99%
Molecular Weight: 327.8
Molecular Formula: C14H17N3O2S•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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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.


References

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

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in water (200 mg/mL), and DMSO (95 mg/mL). Insoluble in ethanol.
Storage :
Store at -20° C
Melting Point :
208-215° C
Boiling Point :
506.2° C at 760 mmHg (Predicted)
Refractive Index :
n20D ~1.62 (Predicted)
IC50 :
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
Ki Data :
ROCK-II: Ki= 0.33 µM; PKA: Ki= 1.6 µM; PKG: Ki= 1.6 µM; PKC: Ki= 3.3 µM; MLCK: Ki= 36 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
HM4031166
PubChem CID :
163751
Merck Index :
14: 3942
MDL Number :
MFCD00943198
SMILES :
C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Cheng Cheng, 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
Date published: 2015-02-05
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