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

MRT00033659 

Cat. No.: HY-117857
Handling Instructions

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.

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MRT00033659 Chemical Structure

MRT00033659 Chemical Structure

CAS No. : 1401731-54-1

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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].

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.

1401731-54-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MRT00033659MRT 00033659MRT-00033659Casein KinaseCheckpoint Kinase (Chk)MDM-2/p53broad-spectrumpyrazolo-pyridineanalogueE2F-1destabilisationInhibitorinhibitorinhibit

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