1401731-54-1

1401731-54-1 structure
1401731-54-1 structure
  • Name: MRT00033659
  • Chemical Name: MRT00033659
  • CAS Number: 1401731-54-1
  • Molecular Formula: C15H14N4O
  • Molecular Weight: 266.30
  • Catalog: Signaling Pathways Apoptosis MDM-2/p53
  • Create Date: 2020-06-01 10:54:06
  • Modify Date: 2024-01-10 17:45:20
  • 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].

Name MRT00033659
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.

Molecular Formula C15H14N4O
Molecular Weight 266.30
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.