1. Cell Cycle/DNA Damage Stem Cell/Wnt Apoptosis
  2. Casein Kinase Checkpoint Kinase (Chk) MDM-2/p53 Early 2 Factor (E2F)
  3. MRT00033659

MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.

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

MRT00033659 Chemical Structure

MRT00033659 Chemical Structure

CAS No. : 1401731-54-1

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
5 mg USD 135 In-stock
10 mg USD 210 In-stock
50 mg USD 550 In-stock
100 mg USD 880 In-stock
200 mg   Get quote  
500 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

Top Publications Citing Use of Products

View All Casein Kinase Isoform Specific Products:

View All Checkpoint Kinase (Chk) Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation[1].

IC50 & Target[1]

CKIδ

0.9 μM (IC50)

Chk1

0.23 μM (IC50)

In Vitro

MRT00033659 (5-40 µM; 48 hours) is sufficient to significantly reduce cell number of 5 µM[1].
MRT00033659 (1-80 µM; 48 hours) induces substantial cell death from 5 µM[1].
MRT00033659 (0.2-80 µM; 48 hours) induces a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 µM to 5 µM[1].
MRT00033659 does not inhibit p38α MAPK[1].

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

Cell Viability Assay[1]

Cell Line: A375 cells
Concentration: 5, 20, 40 µM
Incubation Time: 48 hours
Result: Significantly reduced cell number of 5 µM.

Apoptosis Analysis[1]

Cell Line: A375 cells
Concentration: 1, 5, 10, 20, 40, 80 µM
Incubation Time: 48 hours
Result: Induced substantial cell death from 5 µM.

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 0.2, 1, 5, 10, 20, 40, 80 µM
Incubation Time: 48 hours
Result: Induced a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 µM to 5 µM.
Molecular Weight

266.30

Formula

C15H14N4O

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=NNC2=NC=C(C=C21)C3=CC=CC(NC(C)=O)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (312.92 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 3.7552 mL 18.7758 mL 37.5516 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • 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: ≥ 4.17 mg/mL (15.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 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: ≥ 4.17 mg/mL (15.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 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 compound is unstable in solutions, freshly prepared is recommended.

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. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7552 mL 18.7758 mL 37.5516 mL 93.8791 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL 18.7758 mL
10 mM 0.3755 mL 1.8776 mL 3.7552 mL 9.3879 mL
15 mM 0.2503 mL 1.2517 mL 2.5034 mL 6.2586 mL
20 mM 0.1878 mL 0.9388 mL 1.8776 mL 4.6940 mL
25 mM 0.1502 mL 0.7510 mL 1.5021 mL 3.7552 mL
30 mM 0.1252 mL 0.6259 mL 1.2517 mL 3.1293 mL
40 mM 0.0939 mL 0.4694 mL 0.9388 mL 2.3470 mL
50 mM 0.0751 mL 0.3755 mL 0.7510 mL 1.8776 mL
60 mM 0.0626 mL 0.3129 mL 0.6259 mL 1.5647 mL
80 mM 0.0469 mL 0.2347 mL 0.4694 mL 1.1735 mL
100 mM 0.0376 mL 0.1878 mL 0.3755 mL 0.9388 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
MRT00033659
Cat. No.:
HY-117857
Quantity:
MCE Japan Authorized Agent: