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製品番号: 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 番号: 3076612-97-7
分子式: C₄₄H₄₇N₇O₁₀
分子量:833.88

保管条件:

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

TKP-5 構造式

CAS 番号: 3076612-97-7

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

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).

PROTACs アイソフォーム固有の製品をすべて表示 :

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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.

化学情報

CAS 番号 3076612-97-7
分子量 833.88
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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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Help & FAQs

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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100 mg

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生物活性
- 製品説明
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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TKP-5

PROTACs アイソフォーム固有の製品をすべて表示

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示