TLK1-IN-1
TLK1-IN-1 is a TLK1B inhibitor with a human IC50 of 7.2 μM. TLK1-IN-1 causes accumulation of DNA damage and induces apoptotic cell death in cancer cells. TLK1-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.
For research use only. We do not sell to patients.
- Formula: C24H23BrClN5O3
- Molecular Weight:544.83
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TLK1B 7.2 μM (IC50) |
TLK1-IN-1 (Compound 5n) potently inhibits recombinant TLK1B activity with an IC50 of 7.2 μM using the Nek1 peptide substrate[1].
TLK1-IN-1 (72 小时) is selectively cytotoxic to LNCaP and DU145 prostate cancer cells with GI50 values of 2.7 μM and 6.5 μM, respectively, while showing low toxicity to non-cancerous HEK293 cells[1].
TLK1-IN-1 (5 μM; 72 h) potently suppresses colony formation by LNCaP cells[1].
TLK1-IN-1 (0.2-5 μM; 48 h) inhibits the TLK1 pathway in LNCaP cells, showing dose-dependent inhibition at sub-micromolar concentrations (0.2-1.6 μM)[1].
TLK1-IN-1 (0.5 μM; 36-48 h) plus Bicalutamide (HY-14249) induces DNA damage and apoptosis in LNCaP cells, while TLK1-IN-1 alone increases pro-apoptotic BAX levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP cells
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Concentration:5 μM
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Incubation Time:72 h
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Result:Reduced colony formation by LNCaP cells by 4-fold compared to the positive control.
Resulted in the lowest normalized colony number among tested compounds.
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Cell Line:LNCaP cells
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Concentration:0.2 μM; 0.4 μM; 0.6 μM; 0,8 μM; 1.6 μM; 5 μM
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Incubation Time:48 h
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Result:Reduced pRad9-S328 levels.
Showed a dose-dependent reduction in pRad9-S328 levels at sub-micromolar concentrations (0.2-1.6 μM).
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Cell Line:LNCaP cells
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Concentration:0.5 μM; 0.5 μM plus Bicalutamide (5 μM)
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Incubation Time:48 h
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Result:Increased pH2AX levels by ~4-fold compared to control when combined with 5 μM Bicalutamide.
Increased pro-apoptotic BAX levels by 4-fold compared to control when combined with 5 μM Bicalutamide.
Reduced anti-apoptotic Bcl-2 levels by 6-fold compared to control when combined with 5 μM Bicalutamide.
Increased BAX levels by 2.5-fold compared to control when used alone at 0.5 μM.
Chemical Information
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Molecular Weight 544.83
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Formula C24H23BrClN5O3
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SMILES
O=C(NC1=CC=C(Cl)C=C1)CN(N=C2)C(C3=C2C4=CC(Br)=CC=C4N3CCN5CCOCC5)=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
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Data Sheet (275 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TLK1-IN-1 Related Classifications
HY-173186 Related Classifications
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