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).
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- Pureté: 98.23%
- CAS No.: 3037417-26-5
- Formule: C55H70N8O9
- Masse moléculaire:987.19
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Stockage:
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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] |
In Vitro
TD1092 (0.1-10 μM; 18 h) potently degrades cIAP1, cIAP2, and XIAP without reducing CRBN levels in MCF-7 cells[1].
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].
TD1092 (0.01-1 μM; 18 h) concentration-dependently activates caspase 3/7 in MCF-7 cells[1].
TD1092 (1 μM; 48 h) induces significant levels of apoptotic cell death in MCF-7 cells after 48 h of treatment at 1 μM[1].
TD1092 (0.1 μM; 2 h pre-treatment followed by 3 min TNFα stimulation) potently inhibits TNFα-induced canonical NF-κB and MAPK signaling pathway activation in MCF-7 cells while increasing RIP1 phosphorylation[1].
TD1092 (0.1 μM; 24 h) effectively suppresses TNFα-stimulated migration and invasion of MDA-MB-231 triple-negative breast cancer cells[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.
Chemical Information
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CAS No. 3037417-26-5
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Appearance Solid
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Masse moléculaire 987.19
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 Related Classifications
HY-151966 Related Classifications
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