MRT00033659

Modify Date: 2024-01-10 17:45:20

MRT00033659 Structure
MRT00033659 structure
Common Name MRT00033659
CAS Number 1401731-54-1 Molecular Weight 266.30
Density N/A Boiling Point N/A
Molecular Formula C15H14N4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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[1].

 Names

Name MRT00033659

 MRT00033659 Biological Activity

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].
Related Catalog
Target

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.
References

[1]. Huart AS, et al. A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novelactivator of the p53 pathway. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5578-85.

 Chemical & Physical Properties

Molecular Formula C15H14N4O
Molecular Weight 266.30
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