PARP - TNKS2/PARP5B

XAV 939 is a TNKS inhibitor (IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively).

TC-E 5001 is dual tankyrase (TNKS) inhibitor (Kd values are 79 and 28 nM for TNKS1 and TNKS2 respectively, IC50 = 33 nM for TNKS2) that is devoid of activity at PARP1 and PARP2 (IC50 >19 uM). Inhibits Wnt signaling and stabilizes Axin2 levels.

JW 55 is an inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2).

WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2.

G007-LK displays high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice,

NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2.

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

MN-64 is a potent and selective inhibitor of Tankyrase 1 and 2 (IC50 = 6 and 72 nM, respectively).

Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively).

RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.

G244-LM is a potent and specific tankyrase 1/2 inhibitor that inhibits Wnt signaling.