2. Neuronal Signaling
  3. CaMK
  4. RA306

RA306 is an orally active CaMKIIδ/γ inhibitor with IC50 values of 15, 25, 61, and 420 nM against CaMKIIδ, γ, α, and β isoforms, respectively. RA306 reduces the serine/threonine phosphorylation level of PEAK1, inhibits PEAK1-mediated cancer cell migration and invasion, and attenuates the growth and metastasis of cancer xenografts. RA306 can be used in research related to triple-negative breast cancer and dilated cardiomyopathy.

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

RA306

RA306 Chemical Structure

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

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

RA306 is an orally active CaMKIIδ/γ inhibitor with IC50 values of 15, 25, 61, and 420 nM against CaMKIIδ, γ, α, and β isoforms, respectively. RA306 reduces the serine/threonine phosphorylation level of PEAK1, inhibits PEAK1-mediated cancer cell migration and invasion, and attenuates the growth and metastasis of cancer xenografts. RA306 can be used in research related to triple-negative breast cancer and dilated cardiomyopathy[1][2].

IC50 & Target[2]

CaMK IIδ

15 nM (IC50)

CaMK IIγ

25 nM (IC50)

CaMK IIα

61 nM (IC50)

CaMK IIβ

420 nM (IC50)

In Vitro

RA306 (1 μM; 24 h) significantly inhibits serine/threonine phosphorylation of PEAK1 in MDA-MB-231_EcoR cells stably expressing Flag-tagged PEAK1[1].
RA306 (120 h) reduces the viability of MDA-MB-231_HM cells in a dose-dependent manner in both high-adhesion and ultra-low-adhesion plates[1].
RA306 blocks PEAK1-mediated migration of MDA-MB-231 and MDA-MB-468 cells in transwell migration assays[1].
RA306 blocks PEAK1-mediated invasion of MDA-MB-231 cells in Matrigel chamber invasion assays[1].

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

RA306 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231_EcoR cells stably expressing Flag-tagged PEAK1
Concentration: 1 μM
Incubation Time: 24 h
Result: Significantly inhibited serine/threonine phosphorylation of PEAK1, with relative phosphorylation levels reduced compared to untreated controls.
Parmacokinetics
Species Dose Route Cmax Tmax AUC CL F C0 AUC0-∞ Vss T1/2
Mice[2] 3 mg/kg i.v. / / / 0.490 L/h/kg / 1190 ng/mL 6130 ng·h/mL 3.30 L/kg 5.20 h
Mice[2] 10 mg/kg p.o. 2900 ng/mL 2 h 24800 ng·h/mL 4.32 h 121 % / / / /
In Vivo

RA306 (30 mg/kg; p.o.; once daily for 28 consecutive days) significantly inhibits the growth and lung metastasis of triple-negative breast cancer xenografts in mice, and its therapeutic efficacy is comparable to that of PEAK1 gene knockout[1].
RA306 (30 mg/kg; p.o.; twice daily; 14 days) significantly improves the ejection fraction and cardiac output of α-actin transgenic (TG) mice with dilated cardiomyopathy, via a mechanism of reducing myocardial CaMKII activity by inhibiting PLN threonine-17 phosphorylation[2].
RA306 (30 mg/kg; p.o.; once daily for two months) significantly improves the ejection fraction and cardiac output of α-actin TG mice with advanced dilated cardiomyopathy, and exerts no effect on the detected cardiac remodeling parameters[2].

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

Animal Model: BALB/c athymic nude (6-week-old, female)[1]
Dosage: 30 mg/kg
Administration: p.o.; once daily; 28 days
Result: Attenuated primary tumour growth, with a reduction in total bioluminescent imaging signal comparable to that observed with PEAK1 gene knockout.
Blocked lung metastasis from primary tumours to a similar extent as PEAK1 gene knockout, with a significant reduction in the number of mice exhibiting obvious metastatic growth.
Animal Model: alpha-actin transgenic (TG) mice (8-10 months old, C57BL/6 background, dilated cardiomyopathy model)[2]
Dosage: 30 mg/kg
Administration: p.o.; twice daily; 14 days
Result: Increased ejection fraction from baseline 34.2% to 44.8%.
Increased cardiac output from baseline 13.22 mL/min to 15.60 mL/min.
Caused no notable effect on heart rate.
Significantly inhibited cardiac phospholamban (PLN) phosphorylation at threonine-17.
Caused no significant increase in PLN phosphorylation at serine-16.
Animal Model: alpha-actin transgenic (TG) mice (8 months old, C57BL/6 background, dilated cardiomyopathy model)[2]
Dosage: 30 mg/kg
Administration: p.o.; once daily; 2 months
Result: Significantly increased ejection fraction and cardiac output from baseline at both 2 weeks and 2 months post-treatment initiation.
Caused no notable effect on heart rate or left ventricular internal diameter.
Resulted in minimal to mild focal/multifocal myocardial fibrosis.
Caused no significant difference in heart weight-to-body weight ratio compared to vehicle-treated TG mice.
Showed no signs of myocardial inflammation or cardiomyocyte apoptosis.
Molecular Weight

571.73

Formula

C29H41N5O5S
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=CC(N(CC2)CCC2N3C[C@H](CO)OCC3)=CC=C1NC4=NC=C5C(C(OC(C)C)=C(C(C)(O)C)S5)=N4
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 (174.91 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 1.7491 mL 8.7454 mL 17.4908 mL
5 mM 0.3498 mL 1.7491 mL 3.4982 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
=
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 (4.37 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 (4.37 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: 99.74% ee.: 99.63%

SDS (251 KB)

COA (247 KB) HNMR (145 KB) RP-HPLC (173 KB) NP-HPLC (126 KB) LCMS (240 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 1.7491 mL 8.7454 mL 17.4908 mL 43.7269 mL
5 mM 0.3498 mL 1.7491 mL 3.4982 mL 8.7454 mL
10 mM 0.1749 mL 0.8745 mL 1.7491 mL 4.3727 mL
15 mM 0.1166 mL 0.5830 mL 1.1661 mL 2.9151 mL
20 mM 0.0875 mL 0.4373 mL 0.8745 mL 2.1863 mL
25 mM 0.0700 mL 0.3498 mL 0.6996 mL 1.7491 mL
30 mM 0.0583 mL 0.2915 mL 0.5830 mL 1.4576 mL
40 mM 0.0437 mL 0.2186 mL 0.4373 mL 1.0932 mL
50 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8745 mL
60 mM 0.0292 mL 0.1458 mL 0.2915 mL 0.7288 mL
80 mM 0.0219 mL 0.1093 mL 0.2186 mL 0.5466 mL
100 mM 0.0175 mL 0.0875 mL 0.1749 mL 0.4373 mL
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RA306 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:

RA306RA 306RA-306CaMKCalmodulin-dependent protein kinasesCalmodulin-dependent kinasescalcium/calmodulin-dependent protein kinase II (CaMKII)PEAK1MDA-MB-468 cellsCaMKIIδCaMKIIβdilated cardiomyopathy mouse modelsMDA-MB-231_EcoR cellsCaMKIIγCaMKIIαMDA-MB-231 cellsInhibitorinhibitorinhibit

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