TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor (IC50=69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).
Dual DRAK1 and DRAK2 inhibitor 1 is a potent, dual DRAK2/1 inhibitor Kd value of 9/5 nM, respectively;Dual DRAK1 and DRAK2 inhibitor 1 also is a functional inhibitor of DRAK2/1 enzymatic activity with IC50 of 0.86 and 2.25 uM.Dual DRAK1 and DRAK2 inhibitor 1 is a chemical tool compound to study DRAK1 and DRAK2 biology.
3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division[1][2][3].
PM 02734 is an antineoplastic.
DRAK2-IN-1, compound 16, is a potent, selective and ATP-competitive DRAK2 inhibitor with IC50and Kivalues of 3 nM and 0.26 nM, respectively.DRAK2-IN-1 also has inbitory effect on DRAK1 (IC50=51 nM)[1].
HS56 (Pim-DAPK3 inhibitor HS56) is a potent, dual Pim/DAPK3 inhibitor with Ki of 72 nM (Pim-3) and 315 nM (DAPK3), shows micromolar potency toward Pim-1 and Pim-2 (Ki=1.5 and 17 uM); displays a high degree of selectivity for DAPKs and Pims against a panel of 468 kinases, with only two off-target interactions TYK2 and GAK; also displays no significant inhibition or activation of nicotinic, adrenergic, or muscarinic receptors at 10 uM; HS56 delayed force onset, decreased contractile force, and reduced LC20 phosphorylation in excised rat caudal arterial VSM tissues, lowers blood pressure in spontaneously hypertensive mice without affecting heart rate.
TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer[1].
HS94 (DAPK3 inhibitor HS94) is a selective DAPK3 inhibitor with Ki of 126 nM, >20-fold selectivity over Pim kinases.