TZ1104 is a PROTAC-based CDK7 degrader, with a DC50 of 0.88 nM. TZ1104 forms a ternary complex with VHL E3 ligase and CDK7 to trigger proteasome-dependent CDK7 degradation, destabilizing the CDK7-cyclin H-MAT1 complex. TZ1104 suppresses phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. TZ1104 activates the p53-p21 axis and suppresses oncogenic Myc signaling. TZ1104 induces cell cycle arrest, apoptosis, and differentiation of acute leukemia cells. TZ1104 can be used for the research of acute leukemia[1].
Molecular Weight:
992.69
Formula:
C49H66ClN9O7S2
Target:
Apoptosis,CDK,c-Myc,PROTACs
Application Notes:
MCE Product type: Reference compound
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