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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.



1892595-16-2 HS148 (DAPK3 inhibitor HS148) is a selective DAPK3 inhibitor with Ki of 119 nM, >10-fold selectivity over Pim kinases.


1892594-93-2 HS94 (DAPK3 inhibitor HS94) is a selective DAPK3 inhibitor with Ki of 126 nM, >20-fold selectivity over Pim kinases.


1030203-81-6 HS-38 is a potent and selective DAPK1 and DAPK3 (ZIPK) inhibitor with IC50 of 200 nM for DAPK1 and Kd of 280 nM for ZIPK, also inhibits Pim3 (IC50=200 nM), and displays no activity against Src or Abl, little activity against EGFR; decreases RLC20 phosphorylation in cells, and decreases contractile force generated in mouse aorta, rabbit ileum, and calyculin A stimulated arterial muscle by decreasing RLC20 and MYPT1 phosphorylation; also promotes relaxation in Ca(2+)-sensitized vessels.


871837-60-4 DRAK2-IN-116 is a potent, selective DRAK2 inhibitor with IC50 of 3 nM, shows weak inhibition for DRAK1 (IC50=51 nM) and no significant activity against DAPK1/2/3 (IC50>1 uM).

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