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Kinesore

Cat No.:V23240 Purity: ≥98%
Kinesore is an inhibitor (blocker/antagonist) of the KLC2-SKIP interaction.
Kinesore
Kinesore Chemical Structure CAS No.: 363571-83-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
Other Sizes
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Product Description
Kinesore is an inhibitor (blocker/antagonist) of the KLC2-SKIP interaction.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
It is remarkable that the microtubule network was entirely rearranged into a network of rings and bundles in kinesore-treated cells. Moreover, lysosomal compartments are concentrated in juxtanuclear regions with a low microtubule count. This phenotype was very permeable at 50 μM kinesore; 95±2.4% (n=3, 200 cells total) of the cells had a rearranged non-radial microtubule network. This phenotype was observed in titration tests in cells treated for 1 hour at 25 μM kinesore concentrations; at 12.5 μM doses or lower, the effect was negligible. This impact is reversible since radial microtubule arrays are reconstituted once kinesore is washed out of cells treated with one hour and then for two hours. The microtubule network was shown to be reorganized by kinetin in a panel of cancer and normal mammalian cell lines. 50 μM kinesore causes the microtubule network to reorganize and large microtubule-rich projections to develop in wild-type cells. Kif5B mutant cells showed a substantial suppression of this phenotype, indicating that kinesin-1 is required for the microtubule remodeling caused by kinesore [1].
References

[1]. A small-molecule activator of kinesin-1 drives remodeling of the microtubule network. Proc Natl Acad Sci U S A. 2017 Dec 26;114(52):13738-13743.

Additional Infomation
3,5-Dibromo-N'-((2,5-dimethyl-1-(3-nitrophenyl)-1H-pyrrol-3-yl)methylene)-4-hydroxybenzohydrazide is kinesin-1 modulator
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H16BR2N4O4
Molecular Weight
536.173442840576
Exact Mass
533.953
CAS #
363571-83-9
PubChem CID
5349470
Appearance
Typically exists as solid at room temperature
Density
1.7±0.1 g/cm3
Index of Refraction
1.689
LogP
5.49
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
4
Heavy Atom Count
30
Complexity
649
Defined Atom Stereocenter Count
0
SMILES
BrC1C(=C(C=C(C=1)C(N/N=C\C1C=C(C)N(C2C=CC=C(C=2)[N+](=O)[O-])C=1C)=O)Br)O
InChi Key
DUGCMEGLYHBMAR-AUEPDCJTSA-N
InChi Code
InChI=1S/C20H16Br2N4O4/c1-11-6-14(12(2)25(11)15-4-3-5-16(9-15)26(29)30)10-23-24-20(28)13-7-17(21)19(27)18(22)8-13/h3-10,27H,1-2H3,(H,24,28)/b23-10+
Chemical Name
3,5-dibromo-N-[(E)-[2,5-dimethyl-1-(3-nitrophenyl)pyrrol-3-yl]methylideneamino]-4-hydroxybenzamide
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~125 mg/mL (~233.14 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.08 mg/mL (3.88 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8651 mL 9.3254 mL 18.6508 mL
5 mM 0.3730 mL 1.8651 mL 3.7302 mL
10 mM 0.1865 mL 0.9325 mL 1.8651 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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