| Identification | Back Directory | [Name]
Acetonitrile, 2-[[1-(3-chlorophenyl)-4,5-dihydro-4-oxo-1H-pyrazolo[3,4-d]pyrimidin-6-yl]thio]- | [CAS]
922050-57-5 | [Synonyms]
Pim-DAPK3 inhibitor HS56
Acetonitrile, 2-[[1-(3-chlorophenyl)-4,5-dihydro-4-oxo-1H-pyrazolo[3,4-d]pyrimidin-6-yl]thio]- | [Molecular Formula]
C13H8ClN5OS | [MDL Number]
MFCD32174355 | [MOL File]
922050-57-5.mol | [Molecular Weight]
317.75 |
| Chemical Properties | Back Directory | [Boiling point ]
561.0±60.0 °C(Predicted) | [density ]
1.59±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
-3.25±0.20(Predicted) | [color ]
white to beige | [SMILES]
O=C1NC(SCC#N)=NC2=C1C=NN2C3=CC(Cl)=CC=C3 |
| Hazard Information | Back Directory | [Uses]
HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension[1]. | [Biological Activity]
HS56 is a highly selective and potent dual Pim/DAPK3 inhibitor th at significantly reduces contractile intensity and phosphorylation levels of myosin light chain (LC20) in r at caudal arterial smooth muscle strips. HS56 decreases blood pressure in spontaneously hypertensive mice without affecting heart rate. | [in vivo]
HS56 (10 and 20 mg/kg; i.v.; single injection) decreases blood pressure (BP) in spontaneously hypertensive mice[1]. | Animal Model: | Spontaneously hypertensive renin transgene and wild-type (WT) mice[1] | | Dosage: | 10 and 20 mg/kg | | Administration: | Intravenous injection, single injection | | Result: | Induced dose-dependent decreases in systolic blood pressure. |
| [IC 50]
PIM3: 0.208 μM (Ki); PIM1: 2.94 μM (Ki); PIM2: ＞100 μM (Ki) | [References]
[1] Carlson DA, et, al. Targeting Pim Kinases and DAPK3 to Control Hypertension. Cell Chem Biol. 2018 Oct 18;25(10):1195-1207.e32. DOI:10.1016/j.chembiol.2018.06.006 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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