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H-7, Dihydrochloride (CAS 108930-17-2)

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Synonym:1-(5-Isoquinolinylsulfonyl)-2-methylpiperazine dihydrochloride
Application:An ATP-competitive Ser/Thr kinase inhibitor
CAS Number:108930-17-2
Purity:≥98%
Molecular Weight:364.29
Molecular Formula:C14H17N3O2S•2HCl
Refer to Certificate of Analysis for lot specific data (including water content).
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 Ordering Information
Product NameCatalog #UnitPriceQtyAddFavorites
H-7, Dihydrochloride sc-24009 10 mg $80
H-7, Dihydrochloride sc-24009A 50 mg $310
Description
H-7, Dihydrochloride is a cell-permeable, reversible, ATP-competitive Ser/Thr kinase inhibitor. H-7 is a broad spectrum kinase inhibitor that has been shown to inhibit MYLK (MLCK) (Ki=97 µM), cAMP-dependent protein kinase (PKA) (Ki = 3.0 uM), Protein Kinase C (PKC) (Ki = 6.0 uM), and cGMP-dependent protein kinase (cGKI, PKG) (Ki = 5.8 uM). H-7 inhibits cell invasion and metastasis in B16BL6 cancer cells through the PKC/MEK/ERK pathway. This compound is shown to inhibit Topo I and II in murine L929 cells and induce apoptosis through PKC inhibition.
Technical Information
Physical State:Solid
Solubility:Soluble in water (20 g/l) at 20 °C, 100% ethanol, and DMSO (75 mM).
Storage:Store at -20° C
Melting Point:191-193 °C
Boiling Point:495.3 °C at 760 mmHg (Predicted)
IC50:cAMP-dependent protein kinase, gamma catalytic subunit: IC50 = 3.5 µM (human); cAMP-dependent protein kinase alpha-catalytic subunit: IC50 = 3.5 µM (human); cAMP-dependent protein kinase beta-1 catalytic subunit: IC50 = 3.5 µM (human); Protein kinase C zeta: IC50 = 6 µM (human); Protein kinase C mu: IC50 = 6 µM (human)
Ki Data:MLCK: Ki= 97 µM; PKA: Ki= 3.0 µM; PKC: Ki= 6 µM; PKG: Ki= 5.8 µM
pK Values:pKb: 7.69 (Predicted)
Safety and Reference Information
WGK Germany:3
RTECS:TL9305000
PubChem CID:73332
MDL Number:MFCD00036961
Beilstein Registry:5840763
SMILES:CC1CNCCN1S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl.Cl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
References
1. Kawamoto, S., et al. 1984. Biochem. Biophys. Res. Commun. 125: 258-264. PMID: 6239622
2. Hidaka, H., et al. 1984. Biochemistry. 23: 5036-5041. PMID: 6238627
3. Quick, J., et al. 1992. Biochem. Biophys. Res. Commun. 187: 657-663. PMID: 1530623
4. Baloch, Z., et al. 1995. Cell. Immunol. 160: 98-103. PMID: 7842491
5. Nishida, S., et al. 2003. Life Sci. 74: 781-792. PMID: 14654170
6. Tsubaki, M., et al. 2007. Clin. Exp. Metastasis. 24: 431-438. PMID: 17636410
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