10-4120
THZ1
Größe
£177.00
- SKU:
- 10-4120
- Physischer Zustand:
- Solid
- Molekulargewicht:
- 566.05
- Reinheit:
- 97%
- Aufreinigung:
- HPLC Purified
- Lagerbedingungen:
- -20[o]C
- Hersteller:
- Focus Biomolecules
- CAS Number:
- 1604810-83-4
- Immunogen:
- Kinase
- Weitere Details:
- THZ1 is an irreversible, covalent inhibitor (dual ATP-site and allosteric covalent binding) of CDK7 (IC50 = 15.6nM @ 20min and 3.2nM @ 180 min).1 It displayed broad based antiproliferative activity with IC50's of less than 200nM against 53% of the 1000 cancer cell lines it was tested against. THZ1 disrupts transcription of several proteins including RUNX1, TAL1, and GATA3. It suppresses oncogenic transcription of MYCN-driven cancers.2 THZ1 decreases STAT3 chromatin binding and expression of target genes such as MYC, PIM1, and others in peripheral T-Cell lymphoma cells with the Y640F STAT3 mutation.3 Addition of THZ1 to targeted cancer therapy increases cell death and hinders the development of drug-resistant cell populations in cellular and in vitro cancer models.4
- Versandbedingungen:
- Ambient