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About This Item
Empirical Formula (Hill Notation):
C14H17N3O2S · 2HCl
CAS Number:
Molecular Weight:
364.29
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (TLC)
Form:
lyophilized solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (TLC)
form
lyophilized solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light yellow
solubility
water: 20 mg/mL
storage temp.
2-8°C
SMILES string
[S](=O)(=O)(N3C(CNCC3)C)c1c2c(cncc2)ccc1.[Cl-].[Cl-].[H+].[H+]
InChI
1S/C14H17N3O2S.2ClH/c1-11-9-16-7-8-17(11)20(18,19)14-4-2-3-12-10-15-6-5-13(12)14;;/h2-6,10-11,16H,7-9H2,1H3;2*1H
InChI key
OARGPFMFRLLKPF-UHFFFAOYSA-N
General description
A broad-based, cell-permeable, reversible, ATP-competitive serine-threonine kinase inhibitor. Potent inhibitor of myosin light chain kinase (Ki = 97 µM), protein kinase A (Ki = 3.0 µM), protein kinase C (Ki = 6 µM), and protein kinase G (Ki = 5.8 µM). Induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Also inhibits telomerase activity in quercetin-, H-89-, or herbimycin A-treated NPC-076 cells.
Biochem/physiol Actions
Primary Target
MLCK
MLCK
Target Ki: 3.0 µM, 97 µM, 6.0 µM, 5.8 µM against protein kinase A , myosin light chain kinase, protein kinase C , and protein kinase G, respectively
Preparation Note
Following reconstitution, store in the refrigerator (4°C). Aqueous stock solutions are stable for up to 6 months at 4°C.
Further dilute with aqueous buffers just prior to use.
Other Notes
Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730.
Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.
Bergstrand, H., et al. 1992. J. Pharmacol. Exp. Therap.263, 1334.
Gimond, C., et al. 1992. Exp. Cell Res.203, 365.
Quick, J., et al. 1992. Biochem. Biophys. Res. Commun.187, 657.
Bouli, N.M., and Davis, M. 1990. Brain Res.525, 198.
Takahashi, I., et al. 1990. J. Pharmacol. Exp. Ther.255, 1218.
Schachtele, C., et al. 1988. Biochem. Biophys.Res. Commun.151, 542.
Kawamoto, S., and Hidaka, H. 1984. Biochem. Biophys. Res. Commun.125, 258.
Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.
Bergstrand, H., et al. 1992. J. Pharmacol. Exp. Therap.263, 1334.
Gimond, C., et al. 1992. Exp. Cell Res.203, 365.
Quick, J., et al. 1992. Biochem. Biophys. Res. Commun.187, 657.
Bouli, N.M., and Davis, M. 1990. Brain Res.525, 198.
Takahashi, I., et al. 1990. J. Pharmacol. Exp. Ther.255, 1218.
Schachtele, C., et al. 1988. Biochem. Biophys.Res. Commun.151, 542.
Kawamoto, S., and Hidaka, H. 1984. Biochem. Biophys. Res. Commun.125, 258.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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This item has
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 371955-1MG | 04055977213485 |