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W-7 HCl

SKU: orb1217811

Description

W-7 HCl, a calmodulin antagonist, inhibits Ca2+-calmodulin-dependent myosin light chain kinase and phosphodiesterase, W-7 hydrochloride induces apoptosis and has antitumor activity.

Images & Validation

Key Properties

CAS Number61714-27-0
MW377.32
Purity>98% (HPLC)
FormulaC16H22Cl2N2O2S
SMILESC1=CC2=C(C=CC=C2Cl)C(=C1)S(=O)(=O)NCCCCCCN.Cl
TargetCaMK
SolubilityDMSO:250 mg/mL (662.55 mM; Need ultrasonic)

Bioactivity

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. Animal model: Female BALB/c nu mice (6-week-old) injected with RPMI 8226 cells. Dosage: 3 mg/kg. Administration: Intraperitoneal injection; on 5 consecutive days per week. Result: Significantly reduced tumor growth in a murine MM model.
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. 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. Treatment with W-7 results in the dose-dependent inhibition of cell proliferation in various human multiple myeloma cell lines. W-7induces 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. W-7 competitively inhibits Ca2+/calmodulin-dependent phosphodiesterase with a Ki value of 300 μM.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

W-7 hydrochloride | W-7 hydrochloride | W-7 hydrochloride | W-7 HCl | W 7 HCl | W7 HCl

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    99.75% (May vary between batches)

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    C16H22Cl2N2O2S

    25 mg, 10 mg, 50 mg, 1 ml x 10 mM (in DMSO)
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W-7 HCl (orb1217811)

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