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

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

Cat. No.: HY-107613A Purity: 98.88%
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R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride 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 hydrochloride Chemical Structure

R 59-022 hydrochloride Chemical Structure

CAS No. : 93076-98-3

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10 mg USD 180 In-stock
25 mg USD 360 In-stock
50 mg USD 580 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of R 59-022 hydrochloride:

R 59-022 hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE R 59-022 hydrochloride

View All PKC Isoform Specific Products:

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

View All 5-HT Receptor Isoform Specific Products:

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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

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Description

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

IC50 & Target[4]

PKC

 

serotonin

 

DGK

2.8 μM (IC50)

In Vitro

R 59-022 (10 μM, 1 min) hydrochloride potentiates aggregation, but not shape change induced by sub-maximal concentrations of thrombin[2].
R 59-022 (30 μM, 0-60 min) hydrochloride increases release of Noradrenaline in chromaffin cells[3].
R 59-022 (40 μM, 30 min) hydrochloride activates PKC in HeLa and U87 cells[4].
R 59-022 (0-10 μM, 4 h) hydrochloride blocks EBOV GP-mediated entry into Vero cells[5].

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

R 59-022 hydrochloride 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) hydrochloride 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

496.04

Formula

C27H27ClFN3OS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C(CCN(CC/2)CCC2=C(C3=CC=CC=C3)/C4=CC=C(F)C=C4)=C(C)N=C5N1C=CS5.[H]Cl
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 : 25 mg/mL (50.40 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 2.0160 mL 10.0798 mL 20.1597 mL
5 mM 0.4032 mL 2.0160 mL 4.0319 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 (5.04 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 (5.04 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
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 2.0160 mL 10.0798 mL 20.1597 mL 50.3992 mL
5 mM 0.4032 mL 2.0160 mL 4.0319 mL 10.0798 mL
10 mM 0.2016 mL 1.0080 mL 2.0160 mL 5.0399 mL
15 mM 0.1344 mL 0.6720 mL 1.3440 mL 3.3599 mL
20 mM 0.1008 mL 0.5040 mL 1.0080 mL 2.5200 mL
25 mM 0.0806 mL 0.4032 mL 0.8064 mL 2.0160 mL
30 mM 0.0672 mL 0.3360 mL 0.6720 mL 1.6800 mL
40 mM 0.0504 mL 0.2520 mL 0.5040 mL 1.2600 mL
50 mM 0.0403 mL 0.2016 mL 0.4032 mL 1.0080 mL
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R 59-022 hydrochloride 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 59-02293076-98-3DKGI-IDiacylglycerol kinase inhibitor IPKC5-HT ReceptorProtein kinase CSerotonin Receptor5-hydroxytryptamine ReceptorThrombinplateletsphosphatidicacidneutrophilsfilovirusviralEBOVcancerInhibitorinhibitorinhibit

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