LASSBio-2382
LASSBio-2382 is a dual ROCK1/ROCK2 inhibitor with ROCK1 IC50 of 0.005 μM and ROCK2 IC50 of 0.003 μM. LASSBio-2382 inhibits viability and migration of cancer cells. LASSBio-2382 can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2487752-24-7
- Formula: C18H15N5O
- Molecular Weight:317.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
ROCK1 0.05 μM (IC50) |
ROCK2 0.03 μM (IC50) |
In Vitro
LASSBio-2382 (Compound 17) potently inhibits both purified ROCK1 (IC50 = 0.005 μM) and ROCK2 (IC50 = 0.003 μM) in a cell-free biochemical assay[1].
LASSBio-2382 is insoluble in the PAMPA-BBB assay, precluding measurement of its blood-brain barrier permeability[1].
LASSBio-2382 (30 μM; 24 h) reduces MDA-MB-231 cell viability by 28.8%[1].
LASSBio-2382 (0.1-100 μM; 24 h) inhibits MDA-MB-231 cell migration in a dose-dependent manner, with inhibition reducing wound closure to <50% at 10 μM and <25% at 30 μM, and precipitation observed at 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231 human triple-negative breast adenocarcinoma cells
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Concentration:0.1 μM, 10 μM, 30 μM, 100 μM
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Incubation Time:24 h
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Result:Showed wound closure comparable to the control at 0.1 μM.
Reduced wound closure to less than 50% relative to the control at 10 μM.
Reduced wound closure to below 25% relative to the control at 30 μM.
Showed similar inhibition to 30 μM at 100 μM, with precipitation observed.
Chemical Information
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CAS No. 2487752-24-7
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Molecular Weight 317.34
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Formula C18H15N5O
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SMILES
O=C(CC1=CNC2=C1C=CC=C2)N/N=C/C3=CC(C=NN4)=C4C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)