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  4. D609

D609, an antitumoural xanthate, is a specific and competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor with a Ki of 6.4 μM. D609 is an antioxidative protector and has antiviral and anti-inflammatory activity.

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D609 Chemical Structure

D609 Chemical Structure

CAS No. : 83373-60-8

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Based on 6 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

D609, an antitumoural xanthate, is a specific and competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor with a Ki of 6.4 μM. D609 is an antioxidative protector and has antiviral and anti-inflammatory activity[1][2][3].

IC50 & Target

Ki: 6.4 μM (PC-PLC)
In Vitro

D609 (100 μM; for 2 h) significantly attenuats the proliferation of various cell lines[2].
D609 (50, 100 and 200 μM; for 2 h) results in caspase-3 activation with 200 μM and causes no detectable cleavage with 50, 100 μM[2].
D609 (100 μM; for 2 h) significantly inhibits BrdU incorporation in BV-2 microglia and causes accumulation of cells in G1 phase with decreased number of cells in the S phase[2].
D609 (100 μM; for 2 h and cultured for an additional 2 h or 22 h without D609) increases ceramide levels, up-regulates p21 expression and causes a decreases in phospho-Rb[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

D609 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: RAW 264.7 macrophages, N9 and BV-2 microglia, and DITNC1 astrocytes
Concentration: 100 μM
Incubation Time: For 2 hours
Result: Significantly attenuated the proliferation of RAW 264.7 macrophages, N9 and BV-2 microglia, and DITNC1 astrocytes, without affecting cell viability.

Apoptosis Analysis[2]

Cell Line: BV-2 cells
Concentration: 50, 100 and 200 μM
Incubation Time: For 2 hours
Result: Activated caspase-3 in a dose- and time-dependent manner.

Cell Cycle Analysis[2]

Cell Line: BV-2 cells
Concentration: 100 μM
Incubation Time: For 2 hours
Result: Significantly inhibited BrdU incorporation in BV-2 microglia and caused accumulation of cells in G1 phase with decreased number of cells in the S phase.

Western Blot Analysis[2]

Cell Line: BV-2 cells
Concentration: 100 μM
Incubation Time: For 2 hours
Result: Increased ceramide levels, up-regulated p21 expression and causes a decreased in phospho-Rb.
In Vivo

D609 (2.5, 10 mg/kg/day; ip; for 6 weeks) inhibits the progression of preexisting atherosclerotic lesions in apoE-/- mice and changes the lesion composition into a more stable phenotype[3].
D609 (50 mg/kg; ip; single dose) for 30 min before intratracheal administration of LPS (3 mg/kg) prevents the development of LPS-induced pulmonary hypertension in adult male Wistar rats[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 26-week-old apoE−/− and C57BL/6 WT mice[3]
Dosage: 2.5, 10 mg/kg
Administration: IP; per day for 6 weeks
Result: Inhibited the progression of preexisting atherosclerotic lesions in apoE−/− mice and changed the lesion composition into a more stable phenotype.
Significantly decreased the aortic endothelial expression of the vascular cell adhesion molecule-1 and the intercellular adhesion molecule-1.
Molecular Weight

266.46

Formula

C11H15KOS2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

S=C(OC1C2C3CCCC3C(C1)C2)S[K]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (375.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 2 mg/mL (7.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7529 mL 18.7645 mL 37.5291 mL
5 mM 0.7506 mL 3.7529 mL 7.5058 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (11.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3 mg/mL (11.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 25 mg/mL (93.82 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.7529 mL 18.7645 mL 37.5291 mL 93.8227 mL
5 mM 0.7506 mL 3.7529 mL 7.5058 mL 18.7645 mL
DMSO 10 mM 0.3753 mL 1.8765 mL 3.7529 mL 9.3823 mL
15 mM 0.2502 mL 1.2510 mL 2.5019 mL 6.2548 mL
20 mM 0.1876 mL 0.9382 mL 1.8765 mL 4.6911 mL
25 mM 0.1501 mL 0.7506 mL 1.5012 mL 3.7529 mL
30 mM 0.1251 mL 0.6255 mL 1.2510 mL 3.1274 mL
40 mM 0.0938 mL 0.4691 mL 0.9382 mL 2.3456 mL
50 mM 0.0751 mL 0.3753 mL 0.7506 mL 1.8765 mL
60 mM 0.0625 mL 0.3127 mL 0.6255 mL 1.5637 mL
80 mM 0.0469 mL 0.2346 mL 0.4691 mL 1.1728 mL
100 mM 0.0375 mL 0.1876 mL 0.3753 mL 0.9382 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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D609 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

D60983373-60-8D 609D-609PhospholipaseAntitumouralxanthatephosphatidyl choline-specific phospholipase CPC-PLCantioxidativeantiviralanti-inflammatoryInhibitorinhibitorinhibit

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