Description
HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders.
Product information
CAS Number: 1030203-81-6
Molecular Weight: 349.80
Formula: C14H12ClN5O2S
Chemical Name: 2-{[1-(3-chlorophenyl)-4-oxo-1H, 4H, 5H-pyrazolo[3, 4-d]pyrimidin-6-yl]sulfanyl}propanamide
Smiles: CC(SC1NC(=O)C2C=NN(C=2N=1)C1=CC(Cl)=CC=C1)C(N)=O
InChiKey: NASYEGAVCTZSDO-UHFFFAOYSA-N
InChi: InChI=1S/C14H12ClN5O2S/c1-7(11(16)21)23-14-18-12-10(13(22)19-14)6-17-20(12)9-4-2-3-8(15)5-9/h2-7H,1H3,(H2,16,21)(H,18,19,22)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 7.14 mg/mL (20.41 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
HS38 displays high affinity toward DAPK2, with a Kd of 79 nM. DAPK2 is not implicated in smooth muscle contractility. HS38 significantly reduces relative RLC20 phosphorylation in both the basal and sphingosine 1-phosphate (S1P) activated states in human aortic SM cells. HS38 reduces contractile forces generated by intact mouse aorta in aortic tissue. HS38 reduces the contractile force, RLC20 phosphorylation, and MYPT1 phosphorylation in Ca2+-sensitized rabbit ileum.
References:
- David A Carlson, et al. Fluorescence Linked Enzyme Chemoproteomic Strategy for Discovery of a Potent and Selective DAPK1 and ZIPK Inhibitor. ACS Chem Biol. 2013 Dec 20; 8(12): 2715–2723.
Products are for research use only. Not for human use.
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