TD1092
Based on 1 Customer Validation
TD1092 is a pan-inhibitor of apoptosis protein (IAP) PROTAC degrader that targets cIAP1, cIAP2, and XIAP for degradation. TD1092 induces cell apoptosis by activating caspase. TD1092 inhibits the NF-κB signaling pathway induced by TNFα. TD1092 suppresses TNFα-induced epithelial-mesenchymal transition, cancer cell migration, and invasion. TD1092 is suitable for research on breast cancer, ovarian cancer, melanoma, and inflammation-related diseases.
(Pink: cIAP1 and cIAP2 and XIAP ligand (HY-135997); Blue: Ligands for E3 Ligase ligand (HY-14658); Black: linker).
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 : 98.23%
- CAS 番号: 3037417-26-5
- 分子式: C55H70N8O9
- 分子量:987.19
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
cIAP1 |
cIAP2 |
XIAP |
Caspase 3 |
Caspase-7 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | GI50 |
0.396 μM
Compound: 12; TD-1092
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Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 36410083] |
体外実験
TD1092 (0.1 μM; 0.5-6 h) rapidly degrades the three IAP proteins within 1 hour without affecting CRBN expression in MCF-7 cells[1].
Degradation of IAP proteins induced by TD1092 in MCF-7 cells is strictly dependent on the functional ubiquitin-proteasome system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:0.1 μM; 1 μM; 10 μM
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Incubation Time:18 h
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Result:Potently degraded cIAP1, cIAP2, and XIAP without reducing CRBN levels.
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Cell Line:human breast cancer MCF-7 cells
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Concentration:0.1 μM
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Incubation Time:0.5 h, 1 h, 2 h, 4 h, 6 h
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Result:Induced more than 90% degradation of cIAP1, cIAP2, and XIAP within 1 hour at 0.1 μM.
Maintained unchanged CRBN protein levels across all time points.
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Cell Line:human breast cancer MCF-7 cells
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Concentration:1 μM
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Incubation Time:48 h
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Result:Resulted in 46% of total MCF-7 cells being apoptotic after 48 h of incubation at 1 μM.
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Cell Line:human breast cancer MCF-7 cells
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Concentration:0.1 μM
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Incubation Time:2 h (pre-treatment) + 3 min (TNFα stimulation)
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Result:Significantly reduced TNFα-induced phosphorylation of IKK, IκBα, p65, and p38.
Increased phosphorylation of RIP1, suppressing activation of the canonical NF-κB signaling pathway.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:0.1 μM
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Incubation Time:24 h
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Result:Effectively inhibited the migration and invasion of TNFα-stimulated MDA-MB-231 triple-negative breast cancer cells.
- Scratch/Wound-Healing Migration Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- Cell migration
- Neural Crest/Neuronal Cell Migration Explant Assay
- Research Protocol for Inflammation-related Diseases
- Breast Cancer Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Zigmond Chamber Chemotaxis Assay
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Apoptosis Solutions
- 3D Collagen/Hydrogel Matrix Migration Assay
- Cell invasion
- Cell-Exclusion Zone Migration Assay
- Dunn/Insall Chamber Chemotaxis Assay
化学情報
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CAS 番号 3037417-26-5
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性状 Solid
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分子量 987.19
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分子式 C55H70N8O9
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Color Light yellow to yellow
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SMILES
O=C(N[C@@H]1CCCC2=C1C=CC=C2)[C@H]3N(C([C@@H](NC([C@H](C)NC)=O)C(C)(C)C)=O)CC4=C(C=CC(OCCCCCCCCNC(C(C5)CN5C(C=C6C7=O)=CC=C6C(N7C8CCC(NC8=O)=O)=O)=O)=C4)C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : ≥ 100 mg/mL (101.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). 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 (protect from light). 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 (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0130 mL | 5.0649 mL | 10.1298 mL | 25.3244 mL |
| 5 mM | 0.2026 mL | 1.0130 mL | 2.0260 mL | 5.0649 mL | |
| 10 mM | 0.1013 mL | 0.5065 mL | 1.0130 mL | 2.5324 mL | |
| 15 mM | 0.0675 mL | 0.3377 mL | 0.6753 mL | 1.6883 mL | |
| 20 mM | 0.0506 mL | 0.2532 mL | 0.5065 mL | 1.2662 mL | |
| 25 mM | 0.0405 mL | 0.2026 mL | 0.4052 mL | 1.0130 mL | |
| 30 mM | 0.0338 mL | 0.1688 mL | 0.3377 mL | 0.8441 mL | |
| 40 mM | 0.0253 mL | 0.1266 mL | 0.2532 mL | 0.6331 mL | |
| 50 mM | 0.0203 mL | 0.1013 mL | 0.2026 mL | 0.5065 mL | |
| 60 mM | 0.0169 mL | 0.0844 mL | 0.1688 mL | 0.4221 mL | |
| 80 mM | 0.0127 mL | 0.0633 mL | 0.1266 mL | 0.3166 mL | |
| 100 mM | 0.0101 mL | 0.0506 mL | 0.1013 mL | 0.2532 mL |
TD1092 関連分類
HY-151966 関連分類
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