TKP-5
TKP-5 is a PROTAC protein degrader targeting BRD4. TKP-5 can binds to BRD2, BRD3, BRD4 and BRDT, with Kd values of 150 nM, 100 nM and 150 nM for the first three proteins respectively. TKP-5 inhibits the production of thymic stromal lymphopoietin and suppresses the expression of IL-33 mRNA. TKP-5 is applicable to studies related to tape-stripping induced skin injury.
(Pink: BRD4 ligand (HY-182371); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3076612-97-7
- Formula: C44H47N7O10
- Molecular Weight:833.88
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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
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Biological Activity
TKP-5 (0.1-10 μM; 2-24 h) potently degrades BRD4 in KCMH-1 cells with a DC50 of 16.78 nM, suppresses TSLP production in KCMH-1 cells at concentrations starting at 0.1 μM, binds selectively to the BD1 domains of BRD2, BRD3, BRD4, and BRDT at 1 μM, and forms a stable ternary complex with CRBN and BRD4-BD1 via interactions between its triazole moiety and BRD4's Trp81[1].
TKP-5 (5 h) induces degradation of BRD2, BRD3, and BRD4 in KCMH-1 cells at concentrations below 100 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (male, 8 weeks old, skin barrier disruption model via 10x tape-stripping)[1]
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Dosage:1% (w/w) (80 mg total)
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Administration:topical; single application; 6 hours
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Result:Completely suppressed skin injury-induced IL-33 mRNA expression, with levels reduced to near baseline values and significantly lower than both vehicle control and 1.2% TK-351 ointment groups.
Chemical Information
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CAS No. 3076612-97-7
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Molecular Weight 833.88
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Formula C44H47N7O10
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SMILES
O=C(C)NCCC1=C(C(/C=C/C2=CC=C(OCC3=CN(CCCCCC(NC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)=O)N=N3)C=C2)=O)C=C(OCC)C(OC)=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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