TKP-5 

TKP-5 is a PROTAC protein degrader targeting BRD4. TKP-5 can binds to BRD2, BRD3, BRD4 and BRDT, with K_d 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^[1]. (Pink: BRD4 ligand (HY-182371); Blue: Cereblon ligand (HY-10984); Black: linker).

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.

TKP-5 (1% (w/w); topical; single application; 6 hours) completely inhibits tape-stripping-induced skin injury-related IL-33 mRNA expression in male 8-week-old ICR mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

833.88

C₄₄H₄₇N₇O₁₀

3076612-97-7

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yamakoshi H, et al. Alkyne Two-Phase Strategy: Rapid Generation of TK-285-Derived PROTACs as BRD4 Degraders. J Med Chem. Published online March 19, 2026.  [Content Brief]