371970

HA 1077, Dihydrochloride

A cell-permeable, reversible, and ATP-competitive Ca²⁺ antagonist with anti-vasospastic properties.

• Synonym(s): HA 1077, Dihydrochloride, Fasudil, (5-Isoquinolinesulfonyl)homopiperazine, 2HCl, PKG Inhibitor VII
• Empirical Formula (Hill Notation): C₁₄H₁₇N₃O₂S · 2HCl
• CAS Number: 103745-39-7
• Molecular Weight: 364.29
• MDL number: MFCD00866182
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: white
• solubility: water: 1 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [S](=O)(=O)(N3CCNCCC3)c1c2c(cncc2)ccc1
• InChI: 1S/C14H17N3O2S/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14/h1,3-5,7,11,15H,2,6,8-10H2
• InChI key: NGOGFTYYXHNFQH-UHFFFAOYSA-N

Description

General description

A cell-permeable, reversible, and ATP-competitive Ca²⁺ antagonist with anti-vasospastic properties. Inhibits protein kinase A (K_i = 1.6 µM), protein kinase G (K_i = 1.6 µM), and myosin light chain kinase (K_i = 3.6 µM). Also reported to potently inhibit Rho-associated kinase (ROCK; IC₅₀ = 10.7 µM). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency.

A cell-permeable, reversible, and ATP-competitive Ca²⁺ antagonist with anti-vasospastic properties. Inhibits protein kinase A (K_i = 1.6 µM), protein kinase G (K_i = 1.6 µM), and myosin light chain kinase (K_i = 36 µM). Also reported to potently inhibit Rho-associated kinase (ROCK; IC₅₀ = 10.7 µM). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PKA

Product competes with ATP.

Reversible: yes

Target IC₅₀: 10.7 µM inhibiting Rho-associated kinase (ROCK)

Target K_i: .6 µM, 1.6 µM, 36 µM, inhibiting protein kinase A, protein kinase G, myosin light chain kinase, respectively

Warning

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, refrigerate (4°C). Aqueous stock solutions are stable for up to 6 months at 4°C.

Other Notes

Watanabe, K., et al. 2007. Nature Biotech.25, 681.
Swärd, K., et al. 2000. J. Physiol.522, 33.
Takizawa, S., et al. 1993. Eur. J. Pharmacol. 250, 431.
Seto, M., et al. 1991. Eur. J. Pharmacol.195, 267.
Shirotani, M., et al. 1991. J. Pharmacol. Exp. Ther.259, 738.
Asano, T., et al. 1990. Eur. J. Pharmacol.190, 365.
Sasaki, Y., and Sasaki, Y. 1990. Biochem. Biophys. Res. Commun.171, 1182.
Asano, T., et al. 1989. Br. J. Pharmacol. 98,1091.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable