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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 191089-60-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
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