Catalog No.: PC-49690Not For Human Use, Lab Use Only.
Novobiocin (NVB) is a potent, specific DNA polymerase theta (POLθ, POLQ) inhibitor with IC50 of 24 uM, selectively kills HR-deficient tumor cells in vitro and in vivo.
Novobiocin (NVB) is a potent, specific DNA polymerase theta (POLθ, POLQ) inhibitor with IC50 of 24 uM, selectively kills HR-deficient tumor cells in vitro and in vivo.
Novobiocin displays no activity agaginst six other DNA repair related enzymes HSP90AA1, TRIP13, BLM, RAD51, SMARCAL1 and CHD1.
Novobiocin binds directly and specifically to the POLθ ATPase domain in vitro.
Novobiocin impairs POLθ DNA repair function and phenocopies POLθ depletion in human celsl.
Novobiocin strongly and specifically suppresses the growth of HR-deficient tumors in vivo, Novobiocin (75 mg/kg, via IP, b.i.d.) kills HR-deficient tumors and overrides PARPi resistance in vivo in PDX models.
Novobiocin induces excessive DSB end resection and non-productive RAD51 foci in U2OS cells, overcomes multiple PARPi resistance mechanisms.
