2. Epigenetics TGF-beta/Smad Neuronal Signaling GPCR/G Protein
  3. PKC 5-HT Receptor
  4. R 59-022

R 59-022  (Synonyms: DKGI-I; Diacylglycerol kinase inhibitor I)

Cat. No.: HY-107613 Purity: 99.82%
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R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.

For research use only. We do not sell to patients.

R 59-022 Chemical Structure

R 59-022 Chemical Structure

CAS No. : 93076-89-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 90 In-stock
Solution
10 mM * 1 mL in DMSO USD 90 In-stock
Solid
5 mg USD 89 In-stock
10 mg USD 157 In-stock
25 mg USD 362 In-stock
50 mg USD 615 In-stock
100 mg USD 1030 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of R 59-022:

R 59-022 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE R 59-022

View All PKC Isoform Specific Products:

View All Isoforms
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms
5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4].

IC50 & Target[1][2][3]

PKC

 

serotonin

 

diacylglycerol kinase

2.8 μM (IC50)

In Vitro

R 59-022 (10 μM, 1 min) potentiates platelet aggregation[2].
R 59-022 (30 uM, 0-60 min) increases release of Noradrenaline in chromaffin cells[3].
R 59-022 (40 uM, 30 min) activates PKC in HeLa and U87 cells[4].
R 59-022 (0-10 uM, 4 h) blocks EBOV entry into Vero cells[5].

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

R 59-022 Related Antibodies

Western Blot Analysis[4]

Cell Line: HeLa cells
Concentration: 40 uM
Incubation Time: 30 min
Result: Increased the phosphorylation of PKC downstream targets by about 2.5-fold.
In Vivo

R 59-022 (2 mg/kg, i.p., 12 days) significantly increases median survival in SCID mice implanted with U87 GBM cells[6].

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

Animal Model: SCID mice implanted with U87 GBM cells[6]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Increased median survival and decreased tumor volume.
Molecular Weight

459.58

Formula

C27H26FN3OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(CCN(CC/2)CCC2=C(C3=CC=CC=C3)/C4=CC=C(F)C=C4)=C(C)N=C5N1C=CS5
Shipping

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

DMSO : 62.5 mg/mL (135.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1759 mL 10.8795 mL 21.7590 mL
5 mM 0.4352 mL 2.1759 mL 4.3518 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.

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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: ≥ 2.5 mg/mL (5.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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

Purity: 99.82%

COA (247 KB) HNMR (158 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
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
DMSO 1 mM 2.1759 mL 10.8795 mL 21.7590 mL 54.3975 mL
5 mM 0.4352 mL 2.1759 mL 4.3518 mL 10.8795 mL
10 mM 0.2176 mL 1.0879 mL 2.1759 mL 5.4397 mL
15 mM 0.1451 mL 0.7253 mL 1.4506 mL 3.6265 mL
20 mM 0.1088 mL 0.5440 mL 1.0879 mL 2.7199 mL
25 mM 0.0870 mL 0.4352 mL 0.8704 mL 2.1759 mL
30 mM 0.0725 mL 0.3626 mL 0.7253 mL 1.8132 mL
40 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3599 mL
50 mM 0.0435 mL 0.2176 mL 0.4352 mL 1.0879 mL
60 mM 0.0363 mL 0.1813 mL 0.3626 mL 0.9066 mL
80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6800 mL
100 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5440 mL
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R 59-022 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:

R 59-02293076-89-2DKGI-I Diacylglycerol kinase inhibitor IPKC5-HT ReceptorProtein kinase CSerotonin Receptor5-hydroxytryptamine ReceptorThrombinplateletsphosphatidicacidneutrophilsfilovirusviralEBOVcancerInhibitorinhibitorinhibit

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