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Cat. No.: HY-182370

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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.
(Pink: BRD4 ligand (HY-182371); Blue: Cereblon ligand (HY-10984); Black: linker).

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CAS No.: 3076612-97-7
Formule: C₄₄H₄₇N₇O₁₀
Masse moléculaire:833.88

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

TKP-5 Chemical Structure

CAS No.: 3076612-97-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
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- In Vitro
- In Vivo
Chemical Information
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Activité biologique

Description

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).

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In Vitro

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.

In Vivo

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.

Animal Model:

ICR (male, 8 weeks old, skin barrier disruption model via 10x tape-stripping)^[1]
Dosage:

1% (w/w) (80 mg total)
Administration:

topical; single application; 6 hours
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

CAS No. 3076612-97-7
Masse moléculaire 833.88
Formule C₄₄H₄₇N₇O₁₀
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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TKP-5

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