2. Immunology/Inflammation PI3K/Akt/mTOR Epigenetics Apoptosis
  3. Salt-inducible Kinase (SIK) AMPK Apoptosis
  4. MRT199665

MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.

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MRT199665 Chemical Structure

MRT199665 Chemical Structure

CAS No. : 1456858-57-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 638 In-stock
Solution
10 mM * 1 mL in DMSO USD 638 In-stock
Solid
5 mg USD 580 In-stock
10 mg USD 950 In-stock
25 mg USD 1950 In-stock
50 mg USD 3350 In-stock
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Based on 1 publication(s) in Google Scholar

MRT199665 Related Antibodies

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

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Description

MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively[1]. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells[2]. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370[3].

IC50 & Target

MARK1

2 nM (IC50)

MARK2

2 nM (IC50)

MARK3

3 nM (IC50)

MARK4

2 nM (IC50)

SIK1

110 nM (IC50)

SIK2

12 nM (IC50)

SIK3

43 nM (IC50)

NUAK1

3 nM (IC50)

NUAK2

120 nM (IC50)

AMPKα1

10 nM (IC50)

AMPKα2

10 nM (IC50)

MELK

29 nM (IC50)

TBK1

5400 nM (IC50)

IKKε

7700 nM (IC50)

BRSK2

10000 nM (IC50)

In Vitro

MRT199665 (1 μM; pre-treated for 1 h) increases LPS (100 ng/mL; stimulated for up to 24 h)-stimulated IL-10 mRNA and Nurr77 mRNA production, and IL-10 secretion[1].
MRT199665 (1 nM-100 μM; 48 hours) reduces leukemia growth[2].
MRT199665 treatment can block MEF2C S222 phosphorylation in acute myeloid leukemias (AML) cells. MRT199665 (10 nM-1000 nM; 12 hours) leads to a dose-dependent reduction in total and pS222 MEF2C. MRT199665 also causes a decrease of total MEF2C protein[2].

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

MRT199665 Related Antibodies

Western Blot Analysis[2]

Cell Line: OCI-AML2 and MOLM-13 cells
Concentration: 10, 100, 500, and 1000 nM
Incubation Time: 12 hours
Result: Led to a dose-dependent reduction in total and pS222 MEF2C, causing more than 40% reduction in MEF2C phosphorylation at 10 nM as compared to untreated cells.

Cell Proliferation Assay[2]

Cell Line: Human AML cell lines OCI-AML2, MV4-11, MOLM-13 and Kasumi-1 with endogenous MEF2C phosphorylation; human AML cell lines NB-4, HEL, HL-60 and U937 lacking MEF2C
Concentration: 1 nM, 10 nM, 100n M, 1 μM, 10 μM, 100μM
Incubation Time: 48 hours
Result: Human AML cell lines with endogenous MEF2C phosphorylation (OCI-AML2, MV4–11, MOLM-13 and Kasumi-1) were more sensitive as compared to cell lines lacking MEF2C (NB-4, HEL, HL-60 and U937), with mean IC50 of 26±13 versus 990±29 nM, respectively.
Molecular Weight

469.58

Formula

C28H31N5O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C(C)(C)C2=CN=C(NC3=CC=CC(CN4CCCC4)=C3)N=C2N1[C@H]5CCC6=C5C=CC=C6O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (266.20 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 2.1296 mL 10.6478 mL 21.2956 mL
5 mM 0.4259 mL 2.1296 mL 4.2591 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.08 mg/mL (4.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1296 mL 10.6478 mL 21.2956 mL 53.2391 mL
5 mM 0.4259 mL 2.1296 mL 4.2591 mL 10.6478 mL
10 mM 0.2130 mL 1.0648 mL 2.1296 mL 5.3239 mL
15 mM 0.1420 mL 0.7099 mL 1.4197 mL 3.5493 mL
20 mM 0.1065 mL 0.5324 mL 1.0648 mL 2.6620 mL
25 mM 0.0852 mL 0.4259 mL 0.8518 mL 2.1296 mL
30 mM 0.0710 mL 0.3549 mL 0.7099 mL 1.7746 mL
40 mM 0.0532 mL 0.2662 mL 0.5324 mL 1.3310 mL
50 mM 0.0426 mL 0.2130 mL 0.4259 mL 1.0648 mL
60 mM 0.0355 mL 0.1775 mL 0.3549 mL 0.8873 mL
80 mM 0.0266 mL 0.1331 mL 0.2662 mL 0.6655 mL
100 mM 0.0213 mL 0.1065 mL 0.2130 mL 0.5324 mL
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MRT199665 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:

MRT1996651456858-57-3MRT 199665MRT-199665Salt-inducible Kinase (SIK)AMPKApoptosisAMP-activated protein kinaseAcuteMyeloidleukemiaAMLchemotherapyresistancephosphorylationMARKInhibitorinhibitorinhibit

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