HS56

Research use only, not for human use.

HS56 (Pim-DAPK3 inhibitor HS56) is a potent, dual Pim/DAPK3 inhibitor with Ki of 72 nM (Pim-3) and 315 nM (DAPK3).

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.

Western Blot Analysis Cell Line:VSM tissues Concentration:50 μM Incubation Time:16 hours Result:Modulated LC20 phosphorylation in VSM tissues.

Animal Model:Spontaneously hypertensive renin transgene and wild-type (WT) mice Dosage:10 and 20 mg/kg Administration:Intravenous injection, single injection Result:Induced dose-dependent decreases in systolic blood pressure.

Pim-DAPK3 inhibitor HS56

JAK/STAT Signaling

Pim

Pim

——

——

922050-57-5

317.751

C13H8ClN5OS

>98% (HPLC)

——

N#CCSC1=NC(N(C2=CC=CC(Cl)=C2)N=C3)=C3C(N1)=O

2-((1-(3-chlorophenyl)-4-oxo-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl)thio)acetonitrile

(-20℃)

With Ice Pack

≥ 2 years