Catalog No.: PC-72802Not For Human Use, Lab Use Only.
TAK-981 (TAK981, Subasumstat) is a first-in-class, potent, highly selective SUMO-activating enzyme (SAE) inhibitor with IC50 of 1 nM, >1000-fold selectivity against UAE and NAE.
TAK-981 (TAK981, Subasumstat) is a first-in-class, potent, highly selective SUMO-activating enzyme (SAE) inhibitor with IC50 of 1 nM, >1000-fold selectivity against UAE and NAE.
TAK-981 also exhibits potent and prolonged cellular pathway inhibition with improved selectivity over NAE.
TAK-981 reduces SUMO2/3 conjugation in xenograft tumors following IV administration.
TAK-981 decreased SUMOylation in PDAC cells at the nanomolar range, thereby causing a G2/M cell cycle arrest, mitotic failure and chromosomal segregation defects.
TAK-981 efficiently limited tumour burden in the KPC3 syngeneic mouse model without evidence of systemic toxicity.
In vivo treatment with TAK-981 enhanced the proportions of activated CD8 T cells and natural killer (NK) cells but transiently decreased B cell numbers in tumour, peripheral blood, spleen and lymph nodes.
