2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  3. TLK Apoptosis
  4. 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.

TLK1-IN-1

TLK1-IN-1 Chemical Structure

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TLK1-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

TLK1B

7.2 μM (IC50)

In Vitro

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.

TLK1-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: LNCaP cells
Concentration: 5 μM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 0.2 μM; 0.4 μM; 0.6 μM; 0,8 μM; 1.6 μM; 5 μM
Incubation Time: 48 h
Result: Reduced pRad9-S328 levels.
Showed a dose-dependent reduction in pRad9-S328 levels at sub-micromolar concentrations (0.2-1.6 μM).

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 0.5 μM; 0.5 μM plus Bicalutamide (5 μM)
Incubation Time: 48 h
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.
Molecular Weight

544.83

Formula

C24H23BrClN5O3
SMILES

O=C(NC1=CC=C(Cl)C=C1)CN(N=C2)C(C3=C2C4=CC(Br)=CC=C4N3CCN5CCOCC5)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TLK1-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TLK1-IN-1TLKApoptosisTousled-like kinasemetastatic castration-resistant prostate cancerHEK293TLK1BTousled-like kinase 1DU145BAXNek1 peptide substrateLNCaPprostate cancerTLK1Inhibitorinhibitorinhibit

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