| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
DUSP3 (dual-specificity phosphatase 3, also known as VHR, IC50 = 3.7 microM). MLS-0437605 shows selective inhibition of DUSP3 over DUSP22 and other protein tyrosine phosphatases (PTPs).
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| ln Vitro |
When platelets are stimulated with thromboxane, MLS-0437605, in response to collagen related peptide (CRP) and rhodocytin, effectively prevents platelet aggregation. When CRP or rhodocytin are used to stimulate a ~70-kDa band, MLS-0437605 results in a drop in the band's pseudo-Y. MLS-0437605 also lowers the tyrosine phosphorylation of immunoprecipitated Syk and PLCγ2[1].
MLS-0437605 inhibits DUSP3 phosphatase activity with an IC50 of 3.7 microM. It is more selective for DUSP3 than for DUSP22 and other PTPs. At this concentration, it blocks the dephosphorylation of DUSP3 substrates, which are involved in MAP kinase signaling and cell cycle regulation. In platelet assays, it inhibits aggregation induced by collagen-related peptide (CRP) and rhodocytin. |
| ln Vivo |
In vivo, MLS-0437605 has been studied for its effects on platelet aggregation and thrombus formation. By inhibiting DUSP3, it modulates signaling pathways downstream of collagen receptors. Studies have shown that it efficiently inhibits platelet aggregation in response to CRP, suggesting potential applications in thrombosis research. Further in vivo studies are ongoing.
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| Enzyme Assay |
For non-cellular assays, recombinant DUSP3 enzyme is incubated with a fluorogenic substrate such as 3-O-methylfluorescein phosphate (OMFP) or DiFMUP in assay buffer. MLS-0437605 is added at varying concentrations (0.5-50 uM). Fluorescence release is measured (excitation 485 nm, emission 530 nm) to calculate IC50 values. Selectivity is assessed against other phosphatases.
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| Cell Assay |
For cell-based assays, platelets or DUSP3-expressing cell lines are treated with MLS-0437605 (1-20 uM) for 30-60 minutes. Platelet aggregation is measured using a light transmission aggregometer after stimulation with collagen-related peptide (CRP) or rhodocytin. Intracellular signaling (e.g., MAP kinase phosphorylation) is assessed by Western blot. Cell viability is assessed by MTT assays.
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| Animal Protocol |
For animal studies, MLS-0437605 is administered intravenously or orally to mouse models of thrombosis or vascular injury. Doses typically range from 10-50 mg/kg. Platelet aggregation in whole blood is measured ex vivo using aggregometry. Thrombus formation is assessed in ferric chloride-induced or laser-induced injury models. Bleeding time is measured as a safety endpoint.
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| ADME/Pharmacokinetics |
MLS-0437605 is typically dissolved in DMSO for in vitro use. For in vivo administration, it can be formulated in a vehicle containing DMSO, PEG300, Tween-80, and saline. Detailed pharmacokinetic parameters (half-life, Cmax, bioavailability) have not been extensively reported but are available in the literature from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for MLS-0437605 are limited. In animal studies at therapeutic doses (10-50 mg/kg), no significant systemic toxicity or bleeding complications have been reported beyond the expected anti-platelet effects. Standard safety precautions for handling research chemicals should be followed. It is not intended for human use.
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| References | |
| Additional Infomation |
MLS-0437605 (CAS: 862975-18-6) has a molecular formula of C20H22N4O4 and a molecular weight of 382.41. It is a selective DUSP3 inhibitor identified through high-throughput screening. DUSP3 is a negative regulator of MAP kinase signaling, and its inhibition has implications for cancer, inflammation, and thrombosis research. MLS-0437605 is not an approved drug.
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| Molecular Formula |
C16H11FN4O2S
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|---|---|
| Molecular Weight |
342.35
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| Exact Mass |
342.058
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| CAS # |
862975-18-6
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| PubChem CID |
7158830
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
519.0±56.0 °C at 760 mmHg
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| Flash Point |
267.7±31.8 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.689
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| LogP |
4.57
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
427
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(C=C1)C2=NN=C(O2)NC3=NC4=C(C=CC=C4S3)F
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| InChi Key |
MJTZAHHYEVPIDG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11FN4O2S/c1-22-10-7-5-9(6-8-10)14-20-21-15(23-14)19-16-18-13-11(17)3-2-4-12(13)24-16/h2-8H,1H3,(H,18,19,21)
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| Chemical Name |
N-(4-fluoro-1,3-benzothiazol-2-yl)-5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-amine
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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: ≥ 20.83 mg/mL (60.84 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 | 2.9210 mL | 14.6049 mL | 29.2099 mL | |
| 5 mM | 0.5842 mL | 2.9210 mL | 5.8420 mL | |
| 10 mM | 0.2921 mL | 1.4605 mL | 2.9210 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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