Tz-Thalidomide
Based on 1 Customer Validation
Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research.
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。
- 純度: 98.60%
- CAS 番号: 2087490-42-2
- 分子式: C29H29N7O6
- 分子量:571.58
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
E3 Ligase Ligand-Linker Conjugates アイソフォーム固有の製品をすべて表示
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生物活性
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Cereblon |
Tz-Thalidomide exhibits extremely weak binding to the bromodomains of BRD4-1 and BRD4-2, with IC50 values of 46.25 μM and 62.55 μM, respectively[1].
Tz-Thalidomide (30 μM; 30 min) exhibits extremely weak inhibitory activity against ERK2, showing only 46% inhibition at a concentration of 30 μM[1].
Combined with JQ1-TCO, Tz-Thalidomide (0.1-10 μM; 18 h) induces concentration-dependent degradation of BRD4 in HeLa cells, with complete degradation achieved at concentrations of 10 μM and 3 μM after 18 h of incubation[1].
Combination treatment with Tz-Thalidomide (10 μM; 1-24 h) and JQ1-TCO induces time-dependent degradation of BRD4 in HeLa cells, with complete degradation observable after 24 h of incubation[1].
Combination treatment with Tz-Thalidomide (10 μM; 1-24 h) and Probe 1 induces time-dependent degradation of ERK1/2 in A375 cells, with complete degradation observable after 16 h of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.1-10 μM
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Incubation Time:18 h
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Result:Completely degraded BRD4 at 10 μM and 3 μM.
Partially degraded BRD4 at 1 μM and 0.3 μM.
Did not degrade BRD4 at 0.1 μM.
Did not affect BRD4 levels when administered alone.
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Cell Line:HeLa cells
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Concentration:10 μM
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Incubation Time:1-24 h
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Result:Showed no change in BRD4 levels up to 8 h after addition.
Decreased BRD4 levels visibly by 16 h.
Resulted in undetectable (100% degraded) BRD4 levels by 24 h.
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Cell Line:A375 cells
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Concentration:10 μM
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Incubation Time:1-24 h
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Result:Partially degraded ERK1/2 by 4 h after addition.
Completely degraded ERK1/2 by 16 h.
化学情報
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CAS 番号 2087490-42-2
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性状 Solid
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分子量 571.58
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分子式 C29H29N7O6
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Color Pink to red
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SMILES
O=C(CCCCCOC1=C(C(N(C2CCC(NC2=O)=O)C3=O)=O)C3=CC=C1)NCC(C=C4)=CC=C4C5=NN=C(C)N=N5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (87.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (271 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7495 mL | 8.7477 mL | 17.4954 mL | 43.7384 mL |
| 5 mM | 0.3499 mL | 1.7495 mL | 3.4991 mL | 8.7477 mL | |
| 10 mM | 0.1750 mL | 0.8748 mL | 1.7495 mL | 4.3738 mL | |
| 15 mM | 0.1166 mL | 0.5832 mL | 1.1664 mL | 2.9159 mL | |
| 20 mM | 0.0875 mL | 0.4374 mL | 0.8748 mL | 2.1869 mL | |
| 25 mM | 0.0700 mL | 0.3499 mL | 0.6998 mL | 1.7495 mL | |
| 30 mM | 0.0583 mL | 0.2916 mL | 0.5832 mL | 1.4579 mL | |
| 40 mM | 0.0437 mL | 0.2187 mL | 0.4374 mL | 1.0935 mL | |
| 50 mM | 0.0350 mL | 0.1750 mL | 0.3499 mL | 0.8748 mL | |
| 60 mM | 0.0292 mL | 0.1458 mL | 0.2916 mL | 0.7290 mL | |
| 80 mM | 0.0219 mL | 0.1093 mL | 0.2187 mL | 0.5467 mL |
Tz-Thalidomide 関連分類
HY-101460 関連分類
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