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製品番号: HY-180909

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TMU454

TMU454 is an ASGPR-targeting GalNAc-PROTAC BRD4 degrader conjugate. TMU454 undergoes ASGPR-mediated endocytosis and CTSB cleavage to release MZ1, which selectively degrades BRD4 in ASGPR-positive hepatocellular carcinoma cells via the VHL/UPS/proteasome pathway. TMU454 inhibits cancer cell proliferation and colony formation, and suppresses tumor growth in vivo. TMU454 can be used for research related to hepatocellular carcinoma.
(Pink: BRD4 ligand (HY-13030); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₁₄₂H₂₁₄ClN₂₇O₄₄S₂
分子量:3102.96

保管条件:

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

Data Sheet (302 KB)

TMU454 構造式

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
- IC₅₀ & Target
- 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
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

TMU454 is an ASGPR-targeting GalNAc-PROTAC BRD4 degrader conjugate. TMU454 undergoes ASGPR-mediated endocytosis and CTSB cleavage to release MZ1, which selectively degrades BRD4 in ASGPR-positive hepatocellular carcinoma cells via the VHL/UPS/proteasome pathway. TMU454 inhibits cancer cell proliferation and colony formation, and suppresses tumor growth in vivo. TMU454 can be used for research related to hepatocellular carcinoma^[1]. (Pink: BRD4 ligand (HY-13030); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).

IC₅₀ & Target

^[1]

BRD4

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

TMU454 (0.01-1 μM; 1-24 h) preferentially degrades BRD4 in ASGPR-positive hepatocellular carcinoma cells (HepG2 and Huh7), while showing limited activity in ASGPR-negative cancer cells and normal cells^[1].
TMU454 (1 μM; 12 h)-mediated BRD4 degradation depends on the ubiquitin-proteasome system in HepG2 and Huh7 cells^[1].
TMU454 (1 μM; 12 h)-induced BRD4 degradation is reversible in HepG2 and Huh7 cells^[1].
TMU454 (1 μM; 3 h) degrades BRD4 in HepG2 cells, and this activity is competitively inhibited by the tri-GalNAc ligand and attenuated by the endocytosis inhibitor MβCD, indicating that the entry of TMU454 and BRD4 degradation depend on ASGPR-mediated endocytosis^[1].
TMU454 (48 h) exhibits antiproliferative activity against Huh7 cells with an IC₅₀ of 481.9 nM^[1].
TMU454 (1 μM; 3 days) inhibits the colony formation ability of Huh7 cells^[1].
TMU454 (40 μM; 0.25-4 h) is efficiently cleaved by CTSB in vitro to release MZ1^[1].

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

Western Blot Analysis^[1]

Cell Line:

HepG2, Huh7, DU145, HeLa, and HK-2
Concentration:

0.01, 0.03, 0.1, 0.3, 1 μM (HepG2, Huh7, DU145); 0.1 μM (HepG2, DU145); 0.1, 1 μM (HeLa, HK-2)
Incubation Time:

3 h (HepG2, Huh7, DU145); 1, 3, 6, 12, 24 h (HepG2, DU145); 12 h (HeLa, HK-2)
Result:

Effectively degraded BRD4 in a concentration-dependent manner in ASGPR-positive HepG2 and Huh7 cells and in a time-dependent manner in HepG2 cells.
Exhibited no noticeable BRD4 degradation in ASGPR-negative DU145 cells.
Demonstrated substantially lower BRD4 degradation in normal HK-2 cells.

Western Blot Analysis^[1]

Cell Line:

HepG2 and Huh7
Concentration:

1 μM
Incubation Time:

12 h
Result:

Co-treatment with MG132 completely abolished BRD4 degradation induced by TMU454 in both HepG2 and Huh7 cells.

Western Blot Analysis^[1]

Cell Line:

HepG2 and Huh7
Concentration:

1 μM
Incubation Time:

12 h
Result:

Following compound removal and incubation with fresh medium for an additional 12 h, BRD4 levels in both HepG2 and Huh7 cells were restored.

Western Blot Analysis^[1]

Cell Line:

HepG2
Concentration:

1 μM
Incubation Time:

3 h
Result:

Pretreatment with tri-GalNAc-alkyne significantly impaired TMU454-induced BRD4 degradation in HepG2 cells.\nMβCD substantially reduced TMU454's efficacy in degrading BRD4 in HepG2 cells.\nPretreatment with CA-074Me completely blocked TMU454-induced BRD4 degradation in HepG2 cells.

Cell Proliferation Assay^[1]

Cell Line:

Huh7
Concentration:

1 μM
Incubation Time:

3 days
Result:

Inhibited the colony-forming ability of Huh7 cells.

体内実験

TMU454 (10 mg/kg; i.p.; once daily; 7 days) exhibits potent antitumor activity in a Huh7-derived liver cancer xenograft model with minimal systemic toxicity^[1].

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

Animal Model:

BALB/c nude mice (female, 4 weeks old)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; once daily; 7 days
Result:

Robustly suppressed tumor growth, outperforming the MZ1-treated groups, without inducing notable body weight loss.
Revealed no apparent toxicity in heart, liver, kidney, and spleen.

Related Protocols :

化学情報

分子量 3102.96
分子式 C₁₄₂H₂₁₄ClN₂₇O₄₄S₂
SMILES

OC[C@@H](O1)[C@H](O)[C@H](O)[C@@H](NC(C)=O)[C@@H]1OCCCCC(NCCCNC(CCOCC(COCCC(NCCCNC(CCCCO[C@H]2[C@H](NC(C)=O)[C@@H](O)[C@@H](O)[C@@H](CO)O2)=O)=O)(COCCC(NCCCNC(CCCCO[C@H]3[C@H](NC(C)=O)[C@@H](O)[C@@H](O)[C@@H](CO)O3)=O)=O)NC(CCCC4=CN(N=N4)CCOCCOCCC(N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=O)C(NC(C=C5)=CC=C5COC(O[C@@H](C6)C[C@@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)N6C([C@H](C(C)(C)C)NC(COCCOCCOCCNC(C[C@H](N=C9C(C=C%10)=CC=C%10Cl)C%11=NN=C(C)N%11C%12=C9C(C)=C(C)S%12)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
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

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (302 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Peng Y, et al. Development of Cathepsin B-Responsive GalNAc-PROTACs for Hepatocyte-Targeting Protein Degradation. Journal of medicinal chemistry. 2026 Jan 08;69(1):517-532. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 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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TMU454

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

生物活性

製品説明

IC50 & Target

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

Calculators

Help & FAQs

TMU454 関連分類

HY-180909 関連分類

Bioz

Keywords

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