1. Neuronal Signaling
    Metabolic Enzyme/Protease
    Cytoskeleton
    Apoptosis
  2. CaMK
    Phosphodiesterase (PDE)
    Myosin
    Apoptosis
  3. W-7 hydrochloride

W-7 hydrochloride 

Cat. No.: HY-100912
Handling Instructions

W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis and has antitumor activity.

For research use only. We do not sell to patients.

W-7 hydrochloride Chemical Structure

W-7 hydrochloride Chemical Structure

CAS No. : 61714-27-0

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Description

W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively[1][2]. W-7 hydrochloride induces apoptosis and has antitumor activity[3].

IC50 & Target

IC50: 28 μM (Phosphodiesterase) and 51 µM (Myosin light chain kinase)[1]

In Vitro

W-7 is distributed mainly in the cytoplasm, and inhibits proliferation of Chinese hamster ovary K1 (CHO-K1) cells. W-7 selectively blocks the phase of the cell cycle (G1/S boundary phase) in a manner. 25 μM W-7 arrests the growth of the cells at the G1/S boundary phase of the cell cycle[1].
W-7 (100 μM) exhibits a similar extent of antagonism between the contractile responses to carbachol and KCl. The increase in myosin light chain (P-LC) phosphate content in response to 1-min stimulation with 10 μM carbachol is inhibited by W-7. W-7 antagonizes the smooth muscle contraction through the inhibition of the initial increase in the P-LC phosphorylation[2].
Treatment with W-7 results in the dose-dependent inhibition of cell proliferation in various human multiple myeloma cell lines. W-7 induces G1 phase cell cycle arrest by downregulating cyclins and upregulating p21cip1. W-7 induces apoptosis via caspase activation; this occurred partly through the elevation of intracellular calcium levels and mitochondrial membrane potential depolarization and through inhibition of the STAT3 phosphorylation and subsequent downregulation of Mcl-1 protein[3].
W-7 competitively inhibits Ca2+/calmodulin-dependent phosphodiesterase with a Ki value of 300 μM[4].

In Vivo

W-7 (3 mg/kg; intraperitoneal injection; on 5 consecutive days per week; female BALB/c nu mice) treatment significantly reduces tumor growth in a murine MM model[3].

Animal Model: Female BALB/c nu mice (6-week-old) injected with RPMI 8226 cells[3]
Dosage: 3 mg/kg
Administration: Intraperitoneal injection; on 5 consecutive days per week
Result: Significantly reduced tumor growth in a murine MM model.
Molecular Weight

377.33

Formula

C₁₆H₂₂Cl₂N₂O₂S

CAS No.

61714-27-0

SMILES

O=S(C1=C2C=CC=C(Cl)C2=CC=C1)(NCCCCCCN)=O.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

W-7W7W 7CaMKPhosphodiesterase (PDE)MyosinApoptosisCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesCa2+calmodulinmyosinlightchainphosphateanti-proliferationphosphodiesteraseantitumorInhibitorinhibitorinhibit

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W-7 hydrochloride
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