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K-7174

Catalog No.GC10983

K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.

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K-7174 Chemical Structure

Cas No.: 191089-60-8

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5mg
$78.00
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25mg
$203.00
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500mg
$1,005.00
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1g
$1,803.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Description:

IC50: 9 μM

The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Proteasome inhibition is now considered a unique and effective way to kill cancer cells that can tolerate conventional chemotherapy. K-7174 is a novel orally active proteasome inhibitor.

In vitro: Due to its proteasome inhibitary effect, K-7174 induces transcriptional repression of class I histone deacetylases (HDAC) via caspase-8-dependent degradation of Sp1, the most potent transactivator of class I HDAC genes. HDAC1 overexpression reduces the cytotoxic effect of K-7174 and abrogates histone hyperacetylation without affecting the ubiquitinated protein accumulation in K-7174-treated myeloma cells [1].

In vivo: K-7174 exhibits the therapeutic effects through its anti-proteasome activities, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. In addition, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib [1].

Clinical trial: Up to now, K-7174 is still in the preclinical development stage.

Reference:
[1] Kikuchi J, Yamada S, Koyama D, Wada T, Nobuyoshi M, Izumi T, Akutsu M, Kano Y, Furukawa Y.  The novel orally active proteasome inhibitor K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. J Biol Chem. 2013 Aug 30;288(35):25593-602.

Chemical Properties

Cas No. 191089-60-8 SDF
Chemical Name 1,4-bis((E)-5-(3,4,5-trimethoxyphenyl)pent-4-en-1-yl)-1,4-diazepane dihydrochloride
Canonical SMILES COC1=C(OC)C(OC)=CC(/C([H])=C([H])/CCCN(CC2)CCCN2CCC/C([H])=C([H])/C3=CC(OC)=C(OC)C(OC)=C3)=C1.Cl.Cl
Formula C33H50Cl2N2O6 M.Wt 641.67
Solubility ≥ 64.2mg/mL in Water Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.5584 mL 7.7922 mL 15.5843 mL
5 mM 0.3117 mL 1.5584 mL 3.1169 mL
10 mM 0.1558 mL 0.7792 mL 1.5584 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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