TTBK1/2-IN-3
TTBK1/2-IN-3 (Compound 10) is a potent inhibitor of tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 579 nM and 258 nM, respectively. TTBK1/2-IN-3 inhibits the phosphorylation of TDP-43. TTBK1/2-IN-3 reduces the expression of primary cilia on the surface of iPSCs.
For research use only. We do not sell to patients.
- CAS No.: 2857982-34-2
- Formula: C21H22N4O
- Molecular Weight:346.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
TTBK1/2-IN-3 is a dual inhibitor of the purified kinase domains of TTBK1 and TTBK2, with stronger inhibitory activity against TTBK2 than against TTBK1 (IC50 = 258 nM for TTBK2, IC50 = 579 nM for TTBK1)[1].
TTBK1/2-IN-3 binds to human TTBK1 and TTBK2 in live, intact HEK293 cells, with greater potency against TTBK2 than TTBK1 (IC50 = 4.8 μM for TTBK2, IC50 = 9.1 μM for TTBK1), and exhibits stronger activity in permeabilized cells[1].
TTBK1/2-IN-3 (5 μM; 48 h) reduces phosphorylated and total TDP-43 protein levels in SH-SY5Y neuroblastoma cells[1].
TTBK1/2-IN-3 (0.1-1 μM; 24-72 h) potently inhibits primary cilia formation in human induced pluripotent stem cells (iPSCs) in a time- and dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human SH-SY5Y neuroblastoma cells
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Concentration:5 μM; 0.1, 0.5, 1 μM
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Incubation Time:48 h
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Result:Decreased phospho-TDP-43 expression by ~45% at 5 μM after 48 h compared to untreated controls.
Decreased total TDP-43 expression by ~60% at 5 μM after 48 h compared to untreated controls.
Showed no significant change in total TDP-43 at lower concentrations (0.1, 0.5, 1 μM) after 48 hours.
Chemical Information
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CAS No. 2857982-34-2
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Molecular Weight 346.43
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Formula C21H22N4O
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SMILES
CC(CC)(O)C#CC1=CC2=C(NC3=C2C4=C(C=NC(N)=N4)CCC3)C=C1
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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)
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