2. Epigenetics
  3. Histone Methyltransferase
  4. RK-701

RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A.

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RK-701 Chemical Structure

RK-701 Chemical Structure

CAS No. : 2648855-18-7

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Based on 1 publication(s) in Google Scholar

Other Forms of RK-701:

RK-701 Related Antibodies

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View All Histone Methyltransferase Isoform Specific Products:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A[1].

IC50 & Target[1]

G9a

23-27 nM (IC50)

In Vitro

RK-701 (0.01-3 µM; 4 d) up-regulates the expression level of HbF and γ-globin mRNA without affecting cell viability or erythroid differentiation. RK-701 increases the proportion of HbF expressing cells in a concentration-dependent manner. In HUDEP-2 cells and human primary CD34+ cells, RK-701 also selectively up-regulates the expression level of BGLT3 and reduces the proportion of H3K9me2 in β-globin[1].
RK-701 (1 µM; 4 d) significantly reduces the proportion of BCL11A and ZBTB7A in BGLT3 without increasing the expression of BGLT3 in HUDEP-2 cells under the absence of BCL11A or ZBTB7A[1].

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

RK-701 Related Antibodies

Cell Viability Assay[1]

Cell Line: HUDEP-2 cells and CD34+-derived cells.
Concentration: 0.01, 0.03, 0.1, 0.3, 1 and 3 µM.
Incubation Time: 4 d.
Result: Showed activation for HbF, γ- Globin and BGLT3.

Cell Viability Assay[1]

Cell Line: HUDEP-2 cells.
Concentration: 1 µM.
Incubation Time: 4 d.
Result: Showed inhibition for BCL11A and ZBTB7A.
In Vivo

RK-701 (20 mg/kg and 50 mg/kg; i.p.; 5 weeks, each week for 5 consecutive days) selectively increases mouse embryos ε Y-globin and significantly down-regulates the expression level of H3K9me2 in peripheral blood cells. RK-701 has low toxicity[1].

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

446.54

Formula

C26H30N4O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(C(N[C@@H](CCC2CC2)C(NC3=CC=C(C=C3)C#N)=O)=O)NC(CC(C)(C4)C)=C1C4=O
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 (223.94 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 2.2394 mL 11.1972 mL 22.3944 mL
5 mM 0.4479 mL 2.2394 mL 4.4789 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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 (5.60 mM); Clear solution; Need ultrasonic and warming and heat to 80°C

    This protocol yields a clear solution of 2.5 mg/mL.

    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% Corn Oil

    Solubility: 2.5 mg/mL (5.60 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 2.2394 mL 11.1972 mL 22.3944 mL 55.9860 mL
5 mM 0.4479 mL 2.2394 mL 4.4789 mL 11.1972 mL
10 mM 0.2239 mL 1.1197 mL 2.2394 mL 5.5986 mL
15 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7324 mL
20 mM 0.1120 mL 0.5599 mL 1.1197 mL 2.7993 mL
25 mM 0.0896 mL 0.4479 mL 0.8958 mL 2.2394 mL
30 mM 0.0746 mL 0.3732 mL 0.7465 mL 1.8662 mL
40 mM 0.0560 mL 0.2799 mL 0.5599 mL 1.3997 mL
50 mM 0.0448 mL 0.2239 mL 0.4479 mL 1.1197 mL
60 mM 0.0373 mL 0.1866 mL 0.3732 mL 0.9331 mL
80 mM 0.0280 mL 0.1400 mL 0.2799 mL 0.6998 mL
100 mM 0.0224 mL 0.1120 mL 0.2239 mL 0.5599 mL
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RK-701 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:

RK-7012648855-18-7RK701RK 701Histone MethyltransferaseHbFBGLT3HUDEP-2 cellsInhibitorinhibitorinhibit

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