| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
HS38 targets death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK/DAPK3), which are closely related serine/threonine protein kinases that regulate programmed cell death and phosphorylation of non-muscle and smooth muscle myosin. It is an ATP-competitive inhibitor, meaning it competes with ATP for binding to the kinase domain. HS38 also inhibits PIM3 with an IC50 of 200 nM. By inhibiting these kinases, it modulates cell death pathways and smooth muscle contraction.
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| ln Vitro |
For DAPK2, HS38 has a strong affinity with a Kd of 79 nM. The contractility of smooth muscle is unrelated to DAPK2 [1]. In human aortic SM cells, HS38 dramatically lowers the proportion RLC20 phosphorylation in both the baseline and sphingosine 1-phosphate (S1P) activated states [1]. In aortic tissue, HS38 lessens the contractile force generated by the intact artery aorta [1]. In the Ca2+-sensitized rabbit ileum, HS38 decreases contractility, RLC20 phosphorylation, and MYPT1 phosphorylation [1].
HS38 is a potent and selective inhibitor of DAPK1 and ZIPK with Kd values of 300 nM and 280 nM, respectively. It also inhibits PIM3 with an IC50 of 200 nM. Its activity has been confirmed in various kinase activity assays. The compound provides a lead scaffold for the development of therapeutic agents for smooth muscle-related disorders and a chemical means to probe the function of DAPK1 and ZIPK across species. |
| ln Vivo |
HS38 has been used in the study of smooth muscle-related diseases. Its ability to inhibit DAPK1 and ZIPK, which regulate phosphorylation of smooth muscle myosin, makes it a valuable tool for investigating smooth muscle function and disorders. However, specific in vivo efficacy data in animal models is limited. The compound is primarily used as a research tool.
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| Enzyme Assay |
The primary in vitro assay for HS38 is a kinase activity assay using purified DAPK1, ZIPK, or PIM3 enzymes. The enzymes are incubated with a substrate and ATP in the presence of the compound, and the phosphorylation of the substrate is measured. The Kd values and IC50 are determined from dose-response curves. Selectivity profiling is performed against a panel of kinases.
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| Cell Assay |
Western Blot analysis[1]
Cell Types: CA-VSMC Tested Concentrations: 10 µM Incubation Duration: 40 minutes Experimental Results: Relative RLC20 phosphorylation diminished in basal state and S1P activated state. In vitro cellular experiments for HS38 involve treating cells with the compound and measuring its effects on DAPK1 and ZIPK signaling pathways. The inhibition of kinase activity is assessed by measuring the phosphorylation of downstream targets. The compound's effects on smooth muscle cell contraction, cell death, and other cellular processes can also be evaluated. |
| Animal Protocol |
In vivo animal experiments for HS38 are not extensively documented. As a DAPK1/ZIPK inhibitor, it could be evaluated in animal models of smooth muscle-related disorders, such as hypertension, asthma, or gastrointestinal motility disorders. Its effects on smooth muscle function and disease progression would be assessed.
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| ADME/Pharmacokinetics |
HS38 has a molecular weight of 349.80 g/mol and a molecular formula of C14H12ClN5O2S. It is a small molecule that is typically used as a research reagent. It has a purity of 99.91%. The compound is soluble in DMSO and is stored as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
HS38 is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. As with all research chemicals, standard safety precautions should be followed when handling. Its safety would need to be established for therapeutic applications.
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| References | |
| Additional Infomation |
HS38 is a potent, selective, and ATP-competitive inhibitor of DAPK1 and ZIPK with Kd values of 300 nM and 280 nM, respectively. It also inhibits PIM3 with an IC50 of 200 nM. HS38 is used in the research of smooth muscle-related disorders and provides a chemical means to probe the function of DAPK1 and ZIPK. It is available from various chemical suppliers for research purposes.
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| Molecular Formula |
C14H12CLN5O2S
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| Molecular Weight |
349.793
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| Exact Mass |
349.04
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| CAS # |
1030203-81-6
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| PubChem CID |
135398509
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Index of Refraction |
1.775
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| LogP |
1.27
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
531
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NASYEGAVCTZSDO-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[[1-(3-chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]sulfanyl]propanamide
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| Synonyms |
HS 38; HS-38; HS38
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~7.14 mg/mL (~20.41 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8589 mL | 14.2943 mL | 28.5886 mL | |
| 5 mM | 0.5718 mL | 2.8589 mL | 5.7177 mL | |
| 10 mM | 0.2859 mL | 1.4294 mL | 2.8589 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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