1. Immunology/Inflammation Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  2. Salt-inducible Kinase (SIK) PAK Apoptosis
  3. MRIA9

MRIA9 is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC50 values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively.

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

MRIA9 Chemical Structure

MRIA9 Chemical Structure

CAS No. : 2750707-05-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 792 In-stock
Solution
10 mM * 1 mL in DMSO USD 792 In-stock
Solid
5 mg USD 720 In-stock
10 mg USD 1150 In-stock
25 mg USD 2400 In-stock
50 mg USD 3850 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

MRIA9 is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC50 values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively[1].

IC50 & Target

SIK1

 

SIK2

 

SIK3

 

In Vitro

MRIA9 (5 μM) MRIA9 sensitizes SKOV3 cells to paclitaxel treatment through inducing pronounced apoptosis[1].
MRIA9 (5 μM) with paclitaxel (2 nM) significantly enhances cell death in HeLa cells[1].
MRIA9 strongly impedes centrosome function, causes mitotic spindle mispositioning in ovarian cancer cell lines, prevents the centrosome disjunction during the late G2 phase, and sensitized ovarian cancer cells and patient derived 3D-spheroids to paclitaxel treatment[2].

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

Cell Viability Assay[1]

Cell Line: SKOV3 cells.
Concentration: 0.5-5 μM (1 nM paclitaxel).
Incubation Time: 9 days.
Result: Inhibited cell growth.
In Vivo

MRIA9 shows high oral bioavailability (F = 75-80%)[1].

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

Molecular Weight

496.92

Formula

C24H22ClFN6O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N[C@@H](CO1)CO[C@H]1CN(C2=O)C3=NC(NC)=NC=C3C=C2C4=CC=C(C=C4Cl)C5=NC=CC=C5F

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 : 66.67 mg/mL (134.17 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 2.0124 mL 10.0620 mL 20.1240 mL
5 mM 0.4025 mL 2.0124 mL 4.0248 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    90% Corn Oil

    Solubility: 5 mg/mL (10.06 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

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

    Solubility: ≥ 4.5 mg/mL (9.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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 2.0124 mL 10.0620 mL 20.1240 mL 50.3099 mL
5 mM 0.4025 mL 2.0124 mL 4.0248 mL 10.0620 mL
10 mM 0.2012 mL 1.0062 mL 2.0124 mL 5.0310 mL
15 mM 0.1342 mL 0.6708 mL 1.3416 mL 3.3540 mL
20 mM 0.1006 mL 0.5031 mL 1.0062 mL 2.5155 mL
25 mM 0.0805 mL 0.4025 mL 0.8050 mL 2.0124 mL
30 mM 0.0671 mL 0.3354 mL 0.6708 mL 1.6770 mL
40 mM 0.0503 mL 0.2515 mL 0.5031 mL 1.2577 mL
50 mM 0.0402 mL 0.2012 mL 0.4025 mL 1.0062 mL
60 mM 0.0335 mL 0.1677 mL 0.3354 mL 0.8385 mL
80 mM 0.0252 mL 0.1258 mL 0.2515 mL 0.6289 mL
100 mM 0.0201 mL 0.1006 mL 0.2012 mL 0.5031 mL
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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.

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Product Name:
MRIA9
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HY-139253
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