XDTM13
XDTM13 is a biphenyl amide small-molecule TMPRSS2 inhibitor derived from the lead scaffold Avoralstat (HY-16735), with an IC50 of 3.60 nM. XDTM13 inhibits the autoproteolytic cleavage of TMPRSS2 protein in prostate cancer LNCaP cells and suppresses the migration and invasion ability of LNCaP cells. XDTM13 can be used for research on prostate cancer.
For research use only. We do not sell to patients.
- Formula: C29H30N6O5
- Molecular Weight:542.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
XDTM13 (100 μM; 24 h) blocks TMPRSS2 autoproteolysis in LNCaP cells, increasing full-length TMPRSS2 and reducing its cleaved N-terminal fragment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP
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Concentration:25, 100 μM
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Incubation Time:72 h
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Result:Showed no significant reduction in LNCaP cell viability at 25 μM, yet triggered pronounced viability suppression at 100 μM.
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Cell Line:LNCaP
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Concentration:100 μM
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Incubation Time:24 h
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Result:Resulted in a marked increase in the uncleaved, full-length TMPRSS2 band and a corresponding decrease in the cleaved N-terminal fragment.
Exhibited substantially stronger inhibition of TMPRSS2 autoproteolysis than the other tested compounds.
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Cell Line:LNCaP
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Concentration:25, 100 μM
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Incubation Time:48 h
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Result:Reduced migrated LNCaP cells at both 25 and 100 μM compared with control.
Was more effective than the comparator at inhibiting LNCaP cell migration.
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Cell Line:LNCaP
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Concentration:25, 100 μM
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Incubation Time:48 h
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Result:Reduced invaded LNCaP cells at both 25 and 100 μM compared with control.
Was more effective than the comparator at inhibiting LNCaP cell invasion.
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Cell Line:LNCaP
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Concentration:100 μM
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Incubation Time:0, 24, 48 h
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Result:Showed superior anti-migratory activity, with reduced wound closure at 24 and 48 h.
Chemical Information
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Molecular Weight 542.59
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Formula C29H30N6O5
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SMILES
O=C(O)C1=NC(C(NCC2CC2)=O)=CC=C1C3=CC=C(N4CCOCC4)C=C3C(NC5=CC=C(C(N)=N)C=C5)=O
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XDTM13 Related Classifications
HY-189696 Related Classifications
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